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(→‎Niskocząsteczkowe inhibitory domeny kinazowej JAK2)
 
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Linia 1: Linia 1:
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==Niskocząsteczkowe inhibitory domeny kinazowej JAK2==
+
==Small molecule inhibitors of the tyrosine kinase JAK2==
  
 
{|class="wikitable center" style="text-align:center; font-size:100%; border:1px"
 
{|class="wikitable center" style="text-align:center; font-size:100%; border:1px"
−
! rowspan=2|Lp.
+
! rowspan=2|Nb
−
! rowspan=2|style="background-color:yellow"|inhibitor<br>(inne hamowane kinazy)
+
! rowspan=2|inhibitor<br>(other kinase targets)
−
! rowspan=2|klasa chemiczna
+
! rowspan=2|chemical class
−
! test enzym.
+
! enzymatic test  
−
! colspan=2|test komórkowy
+
! colspan=2|cell test
−
! rowspan=2|literatura
+
! rowspan=2|&nbsp;&nbsp;&nbsp;&nbsp;&nbsp;&nbsp;&nbsp;&nbsp;&nbsp;&nbsp;&nbsp;references&nbsp;&nbsp;&nbsp;&nbsp;&nbsp;&nbsp;&nbsp;&nbsp;&nbsp;&nbsp;&nbsp;
 
|-
 
|-
−
!scope="row"| IC50 (mM)
+
!scope="row"|IC<sub>50</sub> (&micro;M)
−
!scope="row" linia komórkowa
+
!scope="row"|&nbsp;&nbsp;&nbsp;&nbsp;&nbsp;&nbsp;&nbsp;&nbsp;cell&nbsp;line&nbsp;&nbsp;&nbsp;&nbsp;&nbsp;&nbsp;&nbsp;&nbsp;
−
!scope="row" GI50 (mM)
+
!scope="row"|GI<sub>50</sub> (&micro;M)
 
|-
 
|-
 
|1
 
|1
−
!scope="row"|AG490<br>(EGFR, PDGFR)
+
!scope="row" style="background-color:LemonChiffon" |AG490<br>(EGFR, PDGFR)
 
|tyrphostin
 
|tyrphostin
 
|36.4<br>48<br>145.3
 
|36.4<br>48<br>145.3
−
|B-precursor (KOCL-33,-45,-50,-69,KOPN-30bi,-55bi,-57bi,-72bi,KOPN-32,-62,-84,NALM 6)<br>T-precursor (KOPT-K1,-5,-11,Jurkat)<br>Ba/F3:JAK2V617F<br>HEL (JAK2V617F)<br>SET-2 (JAK2V617F/wt)<br>XG-1<br>XG-2<br>U266<br>MDAH2774<br>Caov-3<br>MDA-MB-468
+
|B-precursor (KOCL-33,-45,<br>-50,-69,KOPN-30bi,-55bi,<br>-57bi,-72bi,KOPN-32,-62,<br>-84,NALM 6)<br>T-precursor (KOPT-K1,-5,<br>-11,Jurkat)<br>Ba/F3:JAK2<sup>V617F</sup><br>HEL (JAK2<sup>V617F</sup>)<br>SET-2 (JAK2<sup>V617F/wt</sup>)<br>XG-1<br>XG-2<br>U266<br>MDAH2774<br>Caov-3<br>MDA-MB-468
−
|<br>-<br>-<br>1.0<br>>20.0<br>>20.0<br>14.8<br>12.9<br>26.0<br>-<br>-<br>-
+
|<nowiki>-</nowiki><br><br><br><br>-<br><br>1.0<br>>20.0<br>>20.0<br>14.8<br>12.9<br>26.0<br>-<br>-<br>-
−
|Gazit et al. 1989,1991<br>Meydan et al. 1996<br>Vos et al. 2000<br>Miyamoto et al. 2001<br>Burke et al. 2001<br>Duhé et al. 2002<br>Reddy et al. 2010<br>Jatiani et al. 2010
+
|[http://dx.doi.org/10.1021/jm00130a020 Gazit et al. 1989]<br>[http://dx.doi.org/10.1021/jm00110a022 Gazit et al. 1991]<br>[http://dx.doi.org/10.1038/379645a0 Meydan et al. 1996]<br>[http://dx.doi.org/10.1046/j.1365-2141.2000.02127.x Vos et al. 2000]<br>[http://www.nature.com/leu/journal/v15/n11/full/2402260a.html Miyamoto et al. 2001]<br>[http://www.nature.com/onc/journal/v20/n55/full/1204990a.html Burke et al. 2001]<br>[http://dx.doi.org/10.1023/A%3A1016186907376 Duhé et al. 2002]<br>[http://www.sciencedirect.com/science/article/pii/S0968089610000829 Reddy et al. 2010]<br>[http://gan.sagepub.com/content/1/4/331.abstract Jatiani et al. 2010]
 +
|-
 +
|2
 +
!scope="row" style="background-color:LemonChiffon" |LS104<br>(BCR-ABL)
 +
|tyrphostin
 +
|2.52<br>0.1-0.6
 +
|Ba/F3:EpoR,JAK2<sup>V617F</sup><br>Ba/F3:EpoR,JAK2<sup>wt</sup><br>HEL
 +
|1.5<br>10.0
 +
|[http://bloodjournal.hematologylibrary.org/content/102/12/4153.abstract Grunberger et al. 2003]<br>[http://mct.aacrjournals.org/content/7/5/1176.abstract Lipka et al. 2008]
 +
|-
 +
|3
 +
!scope="row" style="background-color:LemonChiffon" |WP1066
 +
|tyrphostin
 +
|<nowiki>-</nowiki>
 +
|HEL
 +
|2.3
 +
|[http://clincancerres.aacrjournals.org/content/14/3/788.abstract Verstovsek et al. 2008]
 +
|-
 +
|4
 +
!scope="row" style="background-color:LemonChiffon" |ON044580<br>(BCR-ABL)
 +
|&alpha;-benzoyl styryl benzyl sulfide
 +
|0.9-1.2<br>4.2
 +
|Ba/F3:JAK2<sup>V617F</sup><br>HEL<br>SET-2
 +
|0.25<br>0.90<br>3.00
 +
|[http://www.sciencedirect.com/science/article/pii/S0968089610000829 Reddy et al. 2010]<br>[http://gan.sagepub.com/content/1/4/331.abstract Jatiani et al. 2010]<br>[http://gan.sagepub.com/content/1/4/346.abstract Samanta et al. 2010]
 +
|-
 +
|5
 +
!scope="row" style="background-color:LemonChiffon" |lestaurtinib<br>(CEP701)<br>(FLT3,JAK3)
 +
|indolocarbazole
 +
|0.001
 +
|HEL
 +
|0.03-0.10
 +
|[http://bloodjournal.hematologylibrary.org/content/111/12/5663.abstract Hexner et al. 2008]<br>[http://bloodjournal.hematologylibrary.org/content/115/6/1131.abstract Santos et al. 2010]
 +
|-
 +
|6
 +
!scope="row" style="background-color:LemonChiffon" |G&ouml;6976<br>(JAK3, FLT3, PKC&alpha;,&beta;1)
 +
|indolocarbazole
 +
|0.13
 +
|32D<br>32D:TEL-JAK2<br>FDCP1<br>TF-1<br>Mo7E<br>HEL
 +
|0.093<br>0.242<br>-<br>-<br>-<br>-
 +
|[http://dx.doi.org/10.1111/j.1365-2141.2006.06291.x Grandage et al. 2006]
 +
|-
 +
|7
 +
!scope="row" style="background-color:LemonChiffon" |TG02<br>(CDKs, TYK2, FLT3, TYRO3, ERK5, p38&delta;, Fms, Lck, Fyn, JAK1)
 +
|pyrimidine
 +
|<nowiki>-</nowiki>
 +
|HEL<br>SET-2<br>Ba/F3:JAK2<sup>wt</sup><br>Ba/F3:JAK2<sup>V617F</sup><br>Karpas-1106P<br>32D
 +
|0.202<br>0.231<br>0.156<br>0.099<br>0.068<br>0.098
 +
|[http://dx.doi.org/10.1038/leu.2011.218 Goh et al. 2012]<br>[http://dx.doi.org/10.1111/bjh.12018 Pallis et al. 2012]
 +
|-
 +
|8
 +
!scope="row" style="background-color:LemonChiffon" |TG101209<br>(FLT3, RET, JAK3)
 +
|pyrimidine
 +
|0.006
 +
|Ba/F3:JAK2<sup>V617F</sup><br>HEL<br>multiple myeloma cell lines (RPMI8226, MM1S, OPM2, NCI-H929, Dox40, MM1R, LR5)
 +
|0.2<br>2-5<br>-
 +
|[http://dx.doi.org/10.1038/sj.leu.2404750 Pardanani et al. 2007]<br>[http://bloodjournal.hematologylibrary.org/content/114/24/5024.abstract Wang and Fiskus et al. 2009]<br>[http://dx.doi.org/10.1002/ajh.21785 Ramakrishnan et al. 2010]
 +
|-
 +
|9
 +
!scope="row" style="background-color:LemonChiffon" |TG101348<br>(FLT3, RET, JAK1, JAK3, TYK2)
 +
|pyrimidine
 +
|0.003
 +
|Ba/F3:JAK2<sup>V617F</sup><br>HEL
 +
|0.270<br>0.305
 +
|[http://www.sciencedirect.com/science/article/pii/S1535610808000457 Wernig et al. 2008]<br>[http://abstracts.hematologylibrary.org/cgi/content/abstract/ashmtg;114/22/755 Pardanani et al. 2009]<br>[http://jco.ascopubs.org/content/29/7/789.abstract Pardanani et al. 2011]
 +
|-
 +
|10
 +
!scope="row" style="background-color:LemonChiffon" |R723<br>(JAK3, TYK2, FLT3, PRKD2, TBK1, SYK, PAK4, DAPK3, PRKD1, MYLK2, PRKCN, STK22D, IKBKE)
 +
|pyrimidine
 +
|0.002
 +
|Ba/F3:JAK2<sup>V617F</sup>
 +
|0.13-0.20
 +
|[https://ash.confex.com/ash/2009/webprogram/Paper18988.html Shide et al. 2009]<br>[http://bloodjournal.hematologylibrary.org/content/117/25/6866.abstract Shide et al. 2011]
 +
|-
 +
|11
 +
!scope="row" style="background-color:LemonChiffon" |INCB018424<br>(JAK1, JAK3, TYK2)
 +
|pyrrolopyrimidine
 +
|0.0045
 +
|<nowiki>-</nowiki>
 +
|<nowiki>-</nowiki>
 +
|[http://abstracts.hematologylibrary.org/cgi/content/abstract/ashmtg;110/11/3538  Fridman et al. 2007]<br>[http://abstracts.hematologylibrary.org/cgi/content/abstract/ashmtg;110/11/558 Verstovsek et al. 2007]<br>[https://ash.confex.com/ash/2008/webprogram/Paper8625.html Verstovsek et al. 2008]<br>[http://www.nejm.org/doi/full/10.1056/NEJMoa1002028 Verstovsek et al. 2010]<br>[http://bloodjournal.hematologylibrary.org/content/115/15/3109.abstract Quintás-Cardama et al. 2010]<br>[http://dx.doi.org/10.1002/cncr.26129 Mesa et al. 2011]
 +
|-
 +
|12
 +
!scope="row" style="background-color:LemonChiffon" |INCB16562<br>(JAK1, JAK3)
 +
|pyrrolopyrimidine
 +
|0.0003
 +
|Ba/F3:JAK2<sup>V617F</sup><br>Ba/F3:JAK2<sup>K539L</sup><br>Ba/F3:MPL<sup>W515L</sup><br>Ba/F3:TEL-JAK2<br>SET-2<br>UKE-1
 +
|0.177<br>0.406<br>0.600<br>0.168<br>0.046<br>0.573
 +
|[http://bloodjournal.hematologylibrary.org/content/115/14/2919.abstract Koppikar et al. 2010]
 +
|-
 +
|13
 +
!scope="row" style="background-color:LemonChiffon" |CP690550<br>(JAK1, JAK3, TYK2)
 +
|pyrrolopyrimidine
 +
|0.0041<br>0.011<br>0.012<br>0.020
 +
|FDCP-EpoR,JAK2<sup>wt</sup><br>FDCP-EpoR,JAK2<sup>V617F</sup>
 +
|2.1<br>0.25
 +
|[http://search.ebscohost.com/login.aspx?direct=true&db=a9h&AN=11414503&lang=pl&site=eds-live&scope=site Changelian et al. 2003]<br>[http://www.sciencedirect.com/science/article/pii/S0960894X06009152 Chen et al. 2006]<br>[http://www.sciencedirect.com/science/article/pii/S0960894X06014053 Clark et al. 2007]<br>[http://dx.doi.org/10.1111/j.1349-7006.2008.00817.x Manshouri et al. 2008]<br>[http://www.journal-inflammation.com/content/7/1/41 Meyer et al. 2010]<br>[http://dx.doi.org/10.1021/jm101157q Thoma et al. 2011]
 +
|-
 +
|14
 +
!scope="row" style="background-color:LemonChiffon" |AZD1480<br>(JAK1, JAK3, TRKA, AuroraA, FLT4, FGFR1, ARK5)
 +
|pyrazolopyrimidine
 +
|0.0004<br>|0.003
 +
|Ba/F3:TEL-JAK2<br>SET-2<br>UKE1<br>HEL
 +
|0.06<br>0.016<br>0.054<br>0.39
 +
|[http://www.cell.com/cancer-cell/abstract/S1535-6108(09)00384-5 Hedvat et al. 2009]<br>[http://dx.doi.org/10.1021/jm1011319 Ioannidis et al. 2011]
 +
|-
 +
|15
 +
!scope="row" style="background-color:LemonChiffon" |CYT387<br>(JAK1, TYK2, CDK2/cyclinA, JNK1, PRKCN, PRKD1, ROCK2, TBK1)
 +
|aminopyrimidine
 +
|0.018
 +
|Ba/F3:EpoR,JAK2<sup>V617F</sup><br>32D:EpoR,JAK2<sup>V617F</sup><br>HEL<br>TF-1<br>U266<br>CHRF-288-11:JAK2<sup>T875N</sup><br>Ba/F3:TEL-JAK2
 +
|0.5<br>1.5<br>1.5<br>1.25<br>0.75<br>0.001<br>0.724
 +
|[http://dx.doi.org/10.1038/leu.2009.50 Pardanani et al. 2009]<br>[http://bloodjournal.hematologylibrary.org/content/115/25/5232.abstract Tyner et al. 2010]
 +
|-
 +
|16
 +
!scope="row" style="background-color:LemonChiffon" |SGI1252<br>(JAK1, JAK3, TYK2, YES, FLT3, ABL, SRC, LCK)
 +
|diaminopyrimidine
 +
|0.0054<br>0.002<br>0.0197
 +
|FDCP-EpoR,JAK2<sup>wt</sup><br>FDCP-EpoR,JAK2<sup>V617F</sup><br>HEL<br>SET-2<br>UKE-1
 +
|0.074<br>0.110<br>0.441<br>0.055<br>0.089
 +
|[http://linkinghub.elsevier.com/retrieve/pii/S1359634908725059?showall=true Olsen et al. 2008]<br>[https://ash.confex.com/ash/2008/webprogram/Paper10062.html Riaz Ahmed et al. 2008]<br>[http://linkinghub.elsevier.com/retrieve/pii/S0301472X10004947?showall=true Riaz Ahmed et al. 2011]
 +
|-
 +
|17
 +
!scope="row" style="background-color:LemonChiffon" |SB1518<br>(FLT3, JAK1, JAK3, TYK2)
 +
|aminopyrimidine macrocycle
 +
|0.023<br>0.019
 +
|Ba/F3:JAK2<sup>V617F</sup><br>HEL<br>SET-2<br>Karpas-1106P<br>U266
 +
|0.16<br>1.726<br>0.217<br>0.348<br>1.350
 +
|[http://dx.doi.org/10.1038/leu.2011.148 Hart et al. 2011]<br>[http://pubs.acs.org/doi/abs/10.1021/jm200326p William et al. 2011]
 +
|-
 +
|18
 +
!scope="row" style="background-color:LemonChiffon" |"38"<br>(JAK1, TYK2, JAK3, MEKK2, MEKK3)
 +
|8-oxo-pyridopyrimidine
 +
|0.001
 +
|TF-1-EPO (IC<sub>50</sub>)
 +
|0.115
 +
|[http://www.sciencedirect.com/science/article/pii/S0960894X13010226 Labadie et al. 2013]
 +
|-
 +
|19
 +
!scope="row" style="background-color:LemonChiffon" |Z3
 +
|pyridine
 +
|15.0<br>28.0
 +
|HEL
 +
|<nowiki>-</nowiki>
 +
|[http://mct.aacrjournals.org/content/7/8/2308.abstract Sayyah et al. 2008]
 +
|-
 +
|20
 +
!scope="row" style="background-color:LemonChiffon" |"25"<br>(JAK1, GAK, YSK4)
 +
|thienopyridine
 +
|0.002
 +
|Ba/F3:TEL-JAK2 (IC<sub>50</sub>)
 +
|1.62
 +
|[http://dx.doi.org/10.1021/jm200911r Schenkel et al. 2011]
 +
|-
 +
|21
 +
!scope="row" style="background-color:LemonChiffon" |"65"<br>(JAK1, cSRC, TRKA, ACK1, FMS, FYN, FLT3, HCK, RET, BMX, LYN, FGR, LCK, ARK5, BTK, YES, PTK5, TRKB, CaMKII&delta;,&gamma;, PRK2, ARG, MLK1, ALK)
 +
|pyridoindolcarboxamide
 +
|0.0008
 +
|irf1-bla HEL (IC<sub>50</sub>)
 +
|0.025
 +
|[http://dx.doi.org/10.1021/jm200909u Lim et al. 2011]
 +
|-
 +
|22
 +
!scope="row" style="background-color:LemonChiffon" |AT9283<br>(AuroraK, JAK3, FLT3, ABL)
 +
|pyrazole benzimidazole
 +
|0.0012
 +
|HEL (JAK2<sup>V617F</sup>)<br>SET-2 (JAK2<sup>V617F/wt</sup>)<br>Ba/F3:ETV6-JAK2<br>Ba/F3-IL-3<br>TF-1-IL-3<br>CMK (JAK2<sup>A572V</sup>)
 +
|0.110<br>0.057<br>0.016<br>0.017<br>0.040<br>0.026
 +
|[http://dx.doi.org/10.1021/jm800984v Howard et al. 2009]<br>[http://dx.doi.org/10.1111/j.1365-2141.2010.08175.x Dawson et al. 2010]
 +
|-
 +
|23
 +
!scope="row" style="background-color:LemonChiffon" |AZ960<br>(TRKA, AuroraA, ARK5, ALK, CaMKII, FLT4, FGFR1, LIMK1, BrSK2, FAK)
 +
|pyrazole nicotinonitrile
 +
|0.003
 +
|SET-2 (JAK2<sup>V617F/wt</sup>)<br>Ba/F3:TEL-JAK2<br>HTLV-1 infected T cells (MT-1, MT-2)
 +
|0.033<br>0.025<br>-
 +
|[http://www.jbc.org/content/283/47/32334.abstract Gozgit et al. 2008]<br>[http://mct.aacrjournals.org/content/9/12/3386.abstract Yang et al. 2010]
 +
|-
 +
|24
 +
!scope="row" style="background-color:LemonChiffon" |CMP6<br>(JAK1, JAK3, TYK2)
 +
|pyridone tetracycle
 +
|0.001
 +
|CTLL-2<br>B9<br>U266<br>KMS11
 +
|0.052-0.1<br>0.25<br>-<br>-
 +
|[http://www.sciencedirect.com/science/article/pii/S0960894X02001063 Thompson et al. 2002]<br>[http://bloodjournal.hematologylibrary.org/content/107/1/176.abstract Lucet et al. 2006]<br>[http://cancerres.aacrjournals.org/content/66/19/9714.abstract Pedranzini et al. 2006]
 +
|-
 +
|25
 +
!scope="row" style="background-color:LemonChiffon" |"13"
 +
|sulfonamide aminoindazole
 +
|0.078
 +
|<nowiki>-</nowiki>
 +
|<nowiki>-</nowiki>
 +
|[http://www.sciencedirect.com/science/article/pii/S0960894X08010007 Antonysamy et al. 2009]
 +
|-
 +
|26
 +
!scope="row" style="background-color:LemonChiffon" |comp 9<br>(JAK3, ALK, cKIT, GCK)
 +
|polycyclic azaindole
 +
|0.001
 +
|TF-1-GMCSF (IC<sub>50</sub>)<br>HT2-IL2 (IC<sub>50</sub>)
 +
|0.27<br>1.53
 +
|[http://dx.doi.org/10.1021/jm901383u Wang et al. 2009]
 +
|-
 +
|27
 +
!scope="row" style="background-color:LemonChiffon" |"15a"
 +
|polycyclic azaindole
 +
|0.0008
 +
|TF-1-GMCSF (IC<sub>50</sub>)
 +
|0.16
 +
|[http://www.sciencedirect.com/science/article/pii/S0960894X09015911 Wang et al. 2010]
 +
|-
 +
|28
 +
!scope="row" style="background-color:LemonChiffon" |"40"<br>(JAK3)
 +
|aminopyrazolopyrimidine
 +
|0.0002
 +
|TF-1-GMCSF (IC<sub>50</sub>)<br>HT2-IL2 (IC<sub>50</sub>)
 +
|0.16<br>3.2
 +
|[http://www.sciencedirect.com/science/article/pii/S0960894X09014541 Ledeboer et al. 2009]
 +
|-
 +
|29
 +
!scope="row" style="background-color:LemonChiffon" |"29"<br>(JAK1, JAK3)
 +
|pyrrolotriazine aminopyrrazole
 +
|0.0018
 +
|SET-2
 +
|0.11
 +
|[http://www.sciencedirect.com/science/article/pii/S0960894X11000357 Harikrishnan et al. 2011]
 +
|-
 +
|30
 +
!scope="row" style="background-color:LemonChiffon" |atiprimod<br>(JAK3)
 +
|azaspirane
 +
|<nowiki>-</nowiki>
 +
|FDCP-EpoR,JAK2<sup>wt</sup><br>FDCP-EpoR,JAK2<sup>V617F</sup><br>SET-2
 +
|0.69<br>0.42<br>0.53
 +
|[http://bloodjournal.hematologylibrary.org/content/105/11/4470.abstract Hamasaki et al. 2005]<br>[http://dx.doi.org/10.1007/s10637-010-9429-z Quintás-Cardama et al. 2011]
 +
|-
 +
|31
 +
!scope="row" style="background-color:LemonChiffon" |G6
 +
|stilbenoid<br>(diaryleten)
 +
|0.060
 +
|Ba/F3:EpoR,JAK2<sup>V617F</sup><br>HEL
 +
|<nowiki>-</nowiki><br>4.0
 +
|[http://www.sciencedirect.com/science/article/pii/S0960894X09006477 Kiss et al. 2009]<br>[http://www.jbc.org/content/285/41/31399.abstract Majumder et al. 2010]<br>[http://www.jbc.org/content/286/6/4280.abstract Kirabo et al. 2011]
 +
|-
 +
|32
 +
!scope="row" style="background-color:LemonChiffon" |NVP-BSK805<br>(JAK1, TYK2, ABL)
 +
|diarylquinoxaline
 +
|0.00048<br>0.00058<br>0.00056
 +
|Ba/F3:JAK2<sup>V617F</sup><br>SET-2<br>MB-02<br>UKE-1<br>MUTZ-8
 +
|0.039<br>0.051<br>0.064<br>0.071<br>0.331
 +
|[http://mct.aacrjournals.org/content/9/7/1945.abstract Baffert et al. 2010]
 +
|-
 +
|33
 +
!scope="row" style="background-color:LemonChiffon" |"26"<br>(ABL)
 +
|diarylquinoxaline
 +
|0.0073
 +
|SET-2
 +
|0.088
 +
|[http://www.sciencedirect.com/science/article/pii/S0960894X10002568 Pissot-Soldermann et al. 2010]
 +
|-
 +
|34
 +
!scope="row" style="background-color:LemonChiffon" |hexabromo cyclohexane
 +
|cyclohexane
 +
|low &micro;M
 +
|&gamma;-2A
 +
|<nowiki>-</nowiki>
 +
|[http://dx.doi.org/10.1021/jm049470k Sandberg et al. 2005]
 +
|-
 +
|35
 +
!scope="row" style="background-color:LemonChiffon" |XL019<br>(JAK1, JAK3, FLT3, PDGFRB, cKIT)
 +
|arylaminopyrimidine
 +
|0.002
 +
|HEL
 +
|<nowiki>-</nowiki>
 +
|[http://abstracts.hematologylibrary.org/cgi/content/abstract/ashmtg;112/11/2810 Paquette et al. 2008]<br>[http://abstracts.hematologylibrary.org/cgi/content/abstract/ashmtg;112/11/98 Shah et al. 2008]<br>[http://www.sciencedirect.com/science/article/pii/S0960894X12012747 Forsyth et al. 2012]
 +
|-
 +
|36
 +
!scope="row" style="background-color:LemonChiffon" |CEP33779<br>(JAK1, JAK3)
 +
|triazolopyridine
 +
|0.0018
 +
|irf1-bla TF-1 (IC<sub>50</sub>)
 +
|0.061
 +
|[http://dx.doi.org/10.1021/jm300248q Dugan et al. 2012]
 +
|-
 +
|37
 +
!scope="row" style="background-color:LemonChiffon" |"29"<br>(JAK1, JAK3, TYK2)
 +
|triazolopyridine
 +
|0.0017
 +
|SET-2 (IC<sub>50</sub>)
 +
|0.212
 +
|[http://www.sciencedirect.com/science/article/pii/S0960894X13007178 Siu et al. 2013]
 +
|-
 +
|38
 +
!scope="row" style="background-color:LemonChiffon" |"6"<br>(JAK1, JAK3, TYK2)
 +
|imidazopyrrolopyridine
 +
|0.0021
 +
|TF-1-EPO (IC<sub>50</sub>)
 +
|0.097
 +
|[http://dx.doi.org/10.1021/jm300628c Zak et al. 2012]
 +
|-
 +
|39
 +
!scope="row" style="background-color:LemonChiffon" |"7"<br>(JAK1, JAK3, TYK2)
 +
|imidazopyrrolopyridine
 +
|0.0012
 +
|TF-1-EPO (IC<sub>50</sub>)
 +
|0.86
 +
|[http://dx.doi.org/10.1021/jm300438j Kulagowski et al. 2012]
 +
|-
 +
|40
 +
!scope="row" style="background-color:LemonChiffon" |"31"<br>(JAK1, JAK3, TYK2)
 +
|imidazopyrrolopyridine
 +
|0.068
 +
|TF-1-EPO (IC<sub>50</sub>)
 +
|7.68
 +
|[http://dx.doi.org/10.1021/jm4004895 Zak et al. 2013]
 +
|-
 +
|41
 +
!scope="row" style="background-color:LemonChiffon" |"46"<br>(JAK1, TYK2)
 +
|pyridine amide
 +
|0.028
 +
|TF-1-EPO (IC<sub>50</sub>)
 +
|1.7
 +
|[http://www.sciencedirect.com/science/article/pii/S0223523413002304 Liang et al. 2013]
 +
|-
 +
|42
 +
!scope="row" style="background-color:LemonChiffon" |"7j"<br>(JAK1, JAK3, TYK2)
 +
|pyrazolopyrimidine
 +
|0.0001
 +
|SET-2 (IC<sub>50</sub>)<br>TF-1-EPO (IC<sub>50</sub>)
 +
|0.0039<br>0.0074
 +
|[http://dx.doi.org/10.1021/jm3012239 Hanan et al. 2012]
 +
|-
 +
|43
 +
!scope="row" style="background-color:LemonChiffon" |"6"<br>(JAK3)
 +
|pyrazolopyrimidine amine
 +
|0.003
 +
|Ba/F3:TEL-JAK2<br>SET-2<br>UKE1
 +
|0.006<br>0.078<br>0.050
 +
|[http://www.sciencedirect.com/science/article/pii/S0960894X13002989 Guan et al. 2013]
 +
|-
 +
|44
 +
!scope="row" style="background-color:LemonChiffon" |"19a"<br>(JAK1, JAK3, CK2&alpha;2, KDR, ABL, FGR, TRKA, FLT4, FLT3, RET, ALK, FGFR1, AuroraA, LIMK1)
 +
|methylimidazole
 +
|0.002
 +
|Ba/F3:TEL-JAK2<br>SET-2<br>UKE1
 +
|0.012<br>0.014<br>0.055
 +
|[http://dx.doi.org/10.1021/jm401546n Su et al. 2014]
 +
|-
 +
|45
 +
!scope="row" style="background-color:LemonChiffon" |NS-018<br>(JAK1, JAK3, TYK2, SRC, FYN, YES, LYNa, FGR, LCK, HCK, ABL, FLT3)
 +
|pyrazinopyridine diamine
 +
|0.00072
 +
|Ba/F3:JAK2<sup>V617F</sup><br>Ba/F3:TEL-JAK2<br>Ba/F3:MPL<sup>W515L</sup><br>SET-2<br>Ba/F3:TEL-JAK3<br>MV4-11(FLT3-ITD)
 +
|0.060 0.011 0.061 0.120 0.800 0.730
 +
|[http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3255248/ Nakaya et al. 2011]<br>[http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3913942/ Nakaya et al. 2014]
 
|}
 
|}
−
 
−
 
−
2
 
−
LS104
 
−
(BCR-ABL)
 
−
tyrphostin
 
−
2.52
 
−
0.1-0.6
 
−
Ba/F3:EpoR,JAK2V617F
 
−
Ba/F3:EpoR,JAK2wt
 
−
HEL
 
−
1.5
 
−
 
−
10.0
 
−
Grunberger et al. 2003
 
−
Lipka et al. 2008
 
−
3
 
−
WP1066
 
−
tyrphostin
 
−
-
 
−
HEL
 
−
2.3
 
−
Verstovsek et al. 2008
 
−
 
−
4
 
−
ON044580
 
−
(BCR-ABL)
 
−
a-benzoyl styryl benzyl sulfide
 
−
0.9-1.2
 
−
4.2
 
−
Ba/F3:JAK2V617F
 
−
HEL
 
−
SET-2
 
−
0.25
 
−
0.90
 
−
3.00
 
−
Reddy et al. 2010
 
−
Jatiani et al. 2010
 
−
Samanta et al. 2010
 
−
5
 
−
CEP701
 
−
(FLT3,JAK3)
 
−
indolocarbazole
 
−
0.001
 
−
HEL
 
−
0.03-0.10
 
−
Hexner et al. 2008
 
−
Santos et al. 2010
 
−
6
 
−
Go6976
 
−
(JAK3,
 
−
FLT3,
 
−
PKCa,b1)
 
−
indolocarbazole
 
−
0.13
 
−
32D
 
−
32D:TEL-JAK2
 
−
FDCP1
 
−
TF-1
 
−
Mo7E
 
−
HEL
 
−
0.093
 
−
0.242
 
−
-
 
−
-
 
−
-
 
−
-
 
−
Grandage et al. 2006
 
−
7
 
−
TG02
 
−
(CDKs,
 
−
FLT3)
 
−
pyrimidine
 
−
-
 
−
HEL
 
−
SET-2
 
−
Ba/F3:JAK2wt
 
−
Ba/F3:JAK2V617F
 
−
Karpas-1106P
 
−
32D
 
−
0.202
 
−
0.231
 
−
0.156
 
−
0.099
 
−
0.068
 
−
0.098
 
−
Goh et al. 2011
 
−
8
 
−
TG101209
 
−
(FLT3,
 
−
RET,
 
−
JAK3)
 
−
pyrimidine
 
−
0.006
 
−
Ba/F3:JAK2V617F
 
−
HEL
 
−
multiple myeloma cell lines (RPMI8226, MM1S, OPM2, NCI-H929, Dox40, MM1R, LR5)
 
−
0.2
 
−
2-5
 
−
-
 
−
 
−
 
−
 
−
 
−
Pardanani et al. 2007
 
−
Wang and Fiskus et al. 2009
 
−
Ramkrishnan et al. 2010
 
−
9
 
−
TG101348
 
−
(FLT3,RET,JAK1,
 
−
JAK3,TYK2)
 
−
pyrimidine
 
−
0.003
 
−
Ba/F3:JAK2V617F
 
−
HEL
 
−
0.270
 
−
0.305
 
−
Wernig et al. 2008
 
−
Animesh et al. 2009
 
−
Pardanani et al. 2011
 
−
10
 
−
R723
 
−
(JAK3,TYK2,FLT3,
 
−
PRKD2,TBK1,SYK,
 
−
PAK4,DAPK3,PRKD1,MYLK2,PRKCN,
 
−
STK22D,IKBKE)
 
−
pyrimidine
 
−
0.002
 
−
Ba/F3:JAK2V617F
 
−
0.13-0.20
 
−
Shide et al. 2009
 
−
Shide et al. 2011
 
−
11
 
−
INCB018424
 
−
(JAK1,JAK3,TYK2)
 
−
pyrrolopyrimidine
 
−
0.0045
 
−
-
 
−
-
 
−
Verstovsek et al. 2008, 2010
 
−
Mesa 2010
 
−
12
 
−
INCB16562
 
−
(JAK1,JAK3)
 
−
pyrrolopyrimidine
 
−
0.0003
 
−
Ba/F3:JAK2V617F
 
−
Ba/F3:JAK2K539L
 
−
Ba/F3:MPLW515L
 
−
Ba/F3:TEL-JAK2
 
−
SET-2
 
−
UKE-1
 
−
0.177
 
−
0.406
 
−
0.600
 
−
0.168
 
−
0.046
 
−
0.573
 
−
Koppikar et al. 2010
 
−
13
 
−
CP690550
 
−
(JAK1,
 
−
JAK3,
 
−
TYK2)
 
−
pyrrolopyrimidine
 
−
0.0041
 
−
0.011
 
−
0.012
 
−
0.020
 
−
FDCP-EpoR,JAK2wt
 
−
FDCP-EpoR,JAK2V617F
 
−
2.1
 
−
0.25
 
−
Changelian et al. 2003
 
−
Chen et al. 2006
 
−
Clark et al. 2007
 
−
Manshouri et al. 2008
 
−
Meyer et al. 2010
 
−
Thoma et al. 2011
 
−
14
 
−
AZD1480
 
−
(JAK1,JAK3,TRKA,
 
−
AuroraA,FLT4,FGFR1,ARK5)
 
−
pyrazolopyrimidine
 
−
0.0004
 
−
0.003
 
−
Ba/F3:TEL-JAK2
 
−
SET-2
 
−
UKE1
 
−
HEL
 
−
0.06
 
−
0.016
 
−
0.054
 
−
0.39
 
−
Hedvat et al. 2009
 
−
Ioannidis et al. 2011
 
−
15
 
−
CYT387
 
−
(JAK1,TYK2,
 
−
CDK2/cyclinA,
 
−
JNK1,PRKCN,
 
−
PRKD1,ROCK2,TBK1)
 
−
aminopyrimidine
 
−
0.018
 
−
Ba/F3:EpoR,JAK2V617F
 
−
32D:EpoR,JAK2V617F
 
−
HEL
 
−
TF-1
 
−
U266
 
−
CHRF-288-11:JAK2T875N
 
−
Ba/F3:TEL-JAK2
 
−
0.5
 
−
1.5
 
−
1.5
 
−
1.25
 
−
0.75
 
−
0.001
 
−
 
−
0.724
 
−
Pardanani et al. 2009
 
−
Tyner et al. 2010
 
−
16
 
−
SGI1252
 
−
(JAK1,JAK3,TYK2,
 
−
YES,FLT3,ABL,SRC,
 
−
LCK)
 
−
diaminopyrimidine
 
−
0.002
 
−
0.0197
 
−
FDCP-EpoR,JAK2wt
 
−
FDCP-EpoR,JAK2V617F
 
−
HEL
 
−
SET-2
 
−
UKE-1
 
−
0.074
 
−
0.110
 
−
0.441
 
−
0.055
 
−
0.089
 
−
Olsen et al. 2008
 
−
Riaz Ahmed et al. 2011
 
−
17
 
−
SB1518
 
−
(FLT3,JAK1,
 
−
JAK3,TYK2)
 
−
aminopyrimidine macrocycle
 
−
0.023
 
−
0.019
 
−
Ba/F3:JAK2V617F
 
−
HEL
 
−
SET-2
 
−
Karpas-1106P
 
−
U266
 
−
0.16
 
−
1.726
 
−
0.217
 
−
0.348
 
−
1.350
 
−
Hart et al. 2011
 
−
William et al. 2011
 
−
18
 
−
Z3
 
−
pyridine
 
−
15.0
 
−
28.0
 
−
HEL
 
−
-
 
−
Sayyah et al. 2008
 
−
19
 
−
25
 
−
(JAK1,GAK,YSK4)
 
−
thienopyridine
 
−
0.002
 
−
Ba/F3:TEL-JAK2 (IC50)
 
−
1.62
 
−
Schenkel et al. 2011
 
−
20
 
−
65
 
−
(JAK1,cSRC,TRKA,
 
−
ACK1,FMS,FYN,FLT3,HCK,RET,BMX,LYN,
 
−
FGR,LCK,ARK5,BTK,YES,PTK5,TRKB,
 
−
CaMKIId,g,PRK2,ARG,MLK1,ALK)
 
−
pyridoindolcarboxamide
 
−
0.0008
 
−
irf1-bla HEL (IC50)
 
−
0.025
 
−
Lim et al. 2011
 
−
21
 
−
AT9283
 
−
(AuroraK,JAK3, FLT3,ABL)
 
−
pyrazole benzimidazole
 
−
0.0012
 
−
HEL (JAK2V617F)
 
−
SET-2 (JAK2V617F/wt)
 
−
Ba/F3:ETV6-JAK2
 
−
Ba/F3-IL-3
 
−
TF-1-IL-3
 
−
CMK (JAK2A572V)
 
−
0.110
 
−
0.057
 
−
0.016
 
−
0.017
 
−
0.040
 
−
0.026
 
−
Howard et al. 2009
 
−
Dawson et al. 2010
 
−
22
 
−
AZ960
 
−
(TRKA,AuroraA,
 
−
ARK5,ALK,CaMKII,
 
−
FLT4,FGFR1,LIMK1,
 
−
BrSK2,FAK)
 
−
pyrazole nicotinonitrile
 
−
0.003
 
−
SET-2 (JAK2V617F/wt)
 
−
Ba/F3:TEL-JAK2
 
−
HTLV-1 infected T cells (MT-1, MT-2)
 
−
0.033
 
−
0.025
 
−
-
 
−
 
−
Gozgit et al. 2008
 
−
Yang et al. 2010
 
−
23
 
−
CMP6
 
−
(JAK1,
 
−
JAK3,
 
−
TYK2)
 
−
pyridone tetracycle
 
−
0.001
 
−
CTLL-2
 
−
B9
 
−
U266
 
−
KMS11
 
−
0.052-0.1
 
−
0.25
 
−
-
 
−
-
 
−
Thompson et al. 2002
 
−
Lucet et al. 2006
 
−
Pedranzini et al. 2008
 
−
24
 
−
13
 
−
sulfonamide aminoindazole
 
−
0.078
 
−
-
 
−
-
 
−
Antonysamy et al. 2009
 
−
25
 
−
comp 9
 
−
(JAK3,ALK,
 
−
cKIT,GCK)
 
−
polycyclic azaindole
 
−
0.001
 
−
TF-1-GMCSF (IC50)
 
−
HT2-IL2 (IC50)
 
−
0.27
 
−
1.53
 
−
Wang et al. 2009
 
−
26
 
−
15a
 
−
polycyclic azaindole
 
−
0.0008
 
−
TF-1-GMCSF (IC50)
 
−
0.16
 
−
Wang et al. 2010
 
−
27
 
−
40
 
−
(JAK3)
 
−
aminopyrazolopyrimidine
 
−
0.0002
 
−
TF-1-GMCSF (IC50)
 
−
HT2-IL2 (IC50)
 
−
0.16
 
−
3.2
 
−
Ledeboer et al. 2009
 
−
28
 
−
29
 
−
(JAK1,JAK3)
 
−
pyrrolotriazine aminopyrrazole
 
−
0.0018
 
−
SET-2
 
−
0.11
 
−
Harikrishnan et al. 2011
 
−
29
 
−
atiprimod
 
−
(JAK3)
 
−
azaspirane
 
−
-
 
−
FDCP-EpoR,JAK2wt
 
−
FDCP-EpoR,JAK2V617F
 
−
SET-2
 
−
0.69
 
−
0.42
 
−
0.53
 
−
Hamasaki et al. 2005
 
−
Quintás-Cardama et al. 2011
 
−
30
 
−
G6
 
−
stilbenoid
 
−
(diaryleten)
 
−
0.060
 
−
Ba/F3:EpoR,JAK2V617F
 
−
HEL
 
−
-
 
−
 
−
4.0
 
−
Kiss et al. 2009
 
−
Majumder et al. 2010
 
−
Kirabo et al. 2011
 
−
31
 
−
NVP-BSK805
 
−
(JAK1,TYK2,ABL)
 
−
diarylquinoxaline
 
−
0.00048
 
−
0.00058
 
−
0.00056
 
−
Ba/F3:JAK2V617F
 
−
SET-2
 
−
MB-02
 
−
UKE-1
 
−
MUTZ-8
 
−
0.039
 
−
0.051
 
−
0.064
 
−
0.071
 
−
0.331
 
−
Baffert et al. 2010
 
−
32
 
−
26
 
−
(ABL)
 
−
diarylquinoxaline
 
−
0.0073
 
−
SET-2
 
−
0.088
 
−
Pissot-Soldermann et al. 2010
 
−
33
 
−
hexabromo cyclohexane
 
−
hexabromo cyclohexane
 
−
low mM
 
−
g-2A
 
−
-
 
−
Sandberg et al. 2005
 
−
34
 
−
XL019
 
−
(JAK1,JAK3,FLT3,
 
−
PDGFRB,cKIT)
 
−
arylaminopyrimidine
 
−
0.002
 
−
HEL
 
−
-
 
−
Paquette et al. 2008
 
−
Shah et al. 2008
 
−
Forsyth et al. 2012
 
−
35
 
−
CEP33779
 
−
(JAK1,JAK3)
 
−
triazolopyridine
 
−
0.0018
 
−
irf1-bla TF-1 (IC50)
 
−
0.061
 
−
Dugan et al. 2012
 
−
36
 
−
29
 
−
(JAK1,JAK3,TYK2)
 
−
triazolopyridine
 
−
0.0017
 
−
SET-2 (IC50)
 
−
0.212
 
−
Siu et al. 2013
 
−
37
 
−
6
 
−
(JAK1,JAK3,TYK2)
 
−
imidazopyrrolopyridine
 
−
0.0021
 
−
TF-1-EPO (IC50)
 
−
0.097
 
−
Zak et al. 2012
 
−
38
 
−
7
 
−
(JAK1,JAK3,TYK2)
 
−
imidazopyrrolopyridine
 
−
0.0012
 
−
TF-1-EPO (IC50)
 
−
0.86
 
−
Kulagowski et al. 2012
 
−
39
 
−
31
 
−
(JAK1,JAK3,TYK2)
 
−
imidazopyrrolopyridine
 
−
0.068
 
−
TF-1-EPO (IC50)
 
−
7.68
 
−
Zak et al. 2013
 
−
40
 
−
46
 
−
(JAK1,TYK2)
 
−
pyridine amide
 
−
0.028
 
−
TF-1-EPO (IC50)
 
−
1.7
 
−
Liang et al. 2013
 
−
41
 
−
7j
 
−
(JAK1,JAK3,TYK2)
 
−
pyrazolopyrimidine
 
−
0.0001
 
−
SET-2 (IC50)
 
−
TF-1-EPO (IC50)
 
−
0.0039
 
−
0.0074
 
−
Hanan et al. 2012
 
−
42
 
−
6
 
−
(JAK3)
 
−
pyrazolopyrimidine amine
 
−
0.003
 
−
Ba/F3:TEL-JAK2
 
−
SET-2
 
−
UKE1
 
−
0.006
 
−
0.078
 
−
0.050
 
−
Guan et al. 2013
 
−
43
 
−
19a
 
−
(JAK1,JAK3,CK2a2,
 
−
KDR,ABL,FGR,TRKA,FLT4,FLT3,RET,ALK,
 
−
FGFR1,AuroraA,
 
−
LIMK1)
 
−
methylimidazole
 
−
0.002
 
−
Ba/F3:TEL-JAK2
 
−
SET-2
 
−
UKE1
 
−
0.012
 
−
0.014
 
−
0.055
 
−
Su et al. 2014
 

Aktualna wersja na dzień 16:07, 28 lis 2015

Small molecule inhibitors of the tyrosine kinase JAK2

Nb inhibitor
(other kinase targets) 		chemical class enzymatic test cell test            references           
IC50 (µM)         cell line         GI50 (µM)
1 AG490
(EGFR, PDGFR) 		tyrphostin 36.4
48
145.3 		B-precursor (KOCL-33,-45,
-50,-69,KOPN-30bi,-55bi,
-57bi,-72bi,KOPN-32,-62,
-84,NALM 6)
T-precursor (KOPT-K1,-5,
-11,Jurkat)
Ba/F3:JAK2V617F
HEL (JAK2V617F)
SET-2 (JAK2V617F/wt)
XG-1
XG-2
U266
MDAH2774
Caov-3
MDA-MB-468 		-



-

1.0
>20.0
>20.0
14.8
12.9
26.0
-
-
- 		Gazit et al. 1989
Gazit et al. 1991
Meydan et al. 1996
Vos et al. 2000
Miyamoto et al. 2001
Burke et al. 2001
Duhé et al. 2002
Reddy et al. 2010
Jatiani et al. 2010
2 LS104
(BCR-ABL) 		tyrphostin 2.52
0.1-0.6 		Ba/F3:EpoR,JAK2V617F
Ba/F3:EpoR,JAK2wt
HEL 		1.5
10.0 		Grunberger et al. 2003
Lipka et al. 2008
3 WP1066 tyrphostin - HEL 2.3 Verstovsek et al. 2008
4 ON044580
(BCR-ABL) 		α-benzoyl styryl benzyl sulfide 0.9-1.2
4.2 		Ba/F3:JAK2V617F
HEL
SET-2 		0.25
0.90
3.00 		Reddy et al. 2010
Jatiani et al. 2010
Samanta et al. 2010
5 lestaurtinib
(CEP701)
(FLT3,JAK3) 		indolocarbazole 0.001 HEL 0.03-0.10 Hexner et al. 2008
Santos et al. 2010
6 Gö6976
(JAK3, FLT3, PKCα,β1) 		indolocarbazole 0.13 32D
32D:TEL-JAK2
FDCP1
TF-1
Mo7E
HEL 		0.093
0.242
-
-
-
- 		Grandage et al. 2006
7 TG02
(CDKs, TYK2, FLT3, TYRO3, ERK5, p38δ, Fms, Lck, Fyn, JAK1) 		pyrimidine - HEL
SET-2
Ba/F3:JAK2wt
Ba/F3:JAK2V617F
Karpas-1106P
32D 		0.202
0.231
0.156
0.099
0.068
0.098 		Goh et al. 2012
Pallis et al. 2012
8 TG101209
(FLT3, RET, JAK3) 		pyrimidine 0.006 Ba/F3:JAK2V617F
HEL
multiple myeloma cell lines (RPMI8226, MM1S, OPM2, NCI-H929, Dox40, MM1R, LR5) 		0.2
2-5
- 		Pardanani et al. 2007
Wang and Fiskus et al. 2009
Ramakrishnan et al. 2010
9 TG101348
(FLT3, RET, JAK1, JAK3, TYK2) 		pyrimidine 0.003 Ba/F3:JAK2V617F
HEL 		0.270
0.305 		Wernig et al. 2008
Pardanani et al. 2009
Pardanani et al. 2011
10 R723
(JAK3, TYK2, FLT3, PRKD2, TBK1, SYK, PAK4, DAPK3, PRKD1, MYLK2, PRKCN, STK22D, IKBKE) 		pyrimidine 0.002 Ba/F3:JAK2V617F 0.13-0.20 Shide et al. 2009
Shide et al. 2011
11 INCB018424
(JAK1, JAK3, TYK2) 		pyrrolopyrimidine 0.0045 - - Fridman et al. 2007
Verstovsek et al. 2007
Verstovsek et al. 2008
Verstovsek et al. 2010
Quintás-Cardama et al. 2010
Mesa et al. 2011
12 INCB16562
(JAK1, JAK3) 		pyrrolopyrimidine 0.0003 Ba/F3:JAK2V617F
Ba/F3:JAK2K539L
Ba/F3:MPLW515L
Ba/F3:TEL-JAK2
SET-2
UKE-1 		0.177
0.406
0.600
0.168
0.046
0.573 		Koppikar et al. 2010
13 CP690550
(JAK1, JAK3, TYK2) 		pyrrolopyrimidine 0.0041
0.011
0.012
0.020 		FDCP-EpoR,JAK2wt
FDCP-EpoR,JAK2V617F 		2.1
0.25 		Changelian et al. 2003
Chen et al. 2006
Clark et al. 2007
Manshouri et al. 2008
Meyer et al. 2010
Thoma et al. 2011
14 AZD1480
(JAK1, JAK3, TRKA, AuroraA, FLT4, FGFR1, ARK5) 		pyrazolopyrimidine 0.003 Ba/F3:TEL-JAK2
SET-2
UKE1
HEL 		0.06
0.016
0.054
0.39 		Hedvat et al. 2009
Ioannidis et al. 2011
15 CYT387
(JAK1, TYK2, CDK2/cyclinA, JNK1, PRKCN, PRKD1, ROCK2, TBK1) 		aminopyrimidine 0.018 Ba/F3:EpoR,JAK2V617F
32D:EpoR,JAK2V617F
HEL
TF-1
U266
CHRF-288-11:JAK2T875N
Ba/F3:TEL-JAK2 		0.5
1.5
1.5
1.25
0.75
0.001
0.724 		Pardanani et al. 2009
Tyner et al. 2010
16 SGI1252
(JAK1, JAK3, TYK2, YES, FLT3, ABL, SRC, LCK) 		diaminopyrimidine 0.0054
0.002
0.0197 		FDCP-EpoR,JAK2wt
FDCP-EpoR,JAK2V617F
HEL
SET-2
UKE-1 		0.074
0.110
0.441
0.055
0.089 		Olsen et al. 2008
Riaz Ahmed et al. 2008
Riaz Ahmed et al. 2011
17 SB1518
(FLT3, JAK1, JAK3, TYK2) 		aminopyrimidine macrocycle 0.023
0.019 		Ba/F3:JAK2V617F
HEL
SET-2
Karpas-1106P
U266 		0.16
1.726
0.217
0.348
1.350 		Hart et al. 2011
William et al. 2011
18 "38"
(JAK1, TYK2, JAK3, MEKK2, MEKK3) 		8-oxo-pyridopyrimidine 0.001 TF-1-EPO (IC50) 0.115 Labadie et al. 2013
19 Z3 pyridine 15.0
28.0 		HEL - Sayyah et al. 2008
20 "25"
(JAK1, GAK, YSK4) 		thienopyridine 0.002 Ba/F3:TEL-JAK2 (IC50) 1.62 Schenkel et al. 2011
21 "65"
(JAK1, cSRC, TRKA, ACK1, FMS, FYN, FLT3, HCK, RET, BMX, LYN, FGR, LCK, ARK5, BTK, YES, PTK5, TRKB, CaMKIIδ,γ, PRK2, ARG, MLK1, ALK) 		pyridoindolcarboxamide 0.0008 irf1-bla HEL (IC50) 0.025 Lim et al. 2011
22 AT9283
(AuroraK, JAK3, FLT3, ABL) 		pyrazole benzimidazole 0.0012 HEL (JAK2V617F)
SET-2 (JAK2V617F/wt)
Ba/F3:ETV6-JAK2
Ba/F3-IL-3
TF-1-IL-3
CMK (JAK2A572V) 		0.110
0.057
0.016
0.017
0.040
0.026 		Howard et al. 2009
Dawson et al. 2010
23 AZ960
(TRKA, AuroraA, ARK5, ALK, CaMKII, FLT4, FGFR1, LIMK1, BrSK2, FAK) 		pyrazole nicotinonitrile 0.003 SET-2 (JAK2V617F/wt)
Ba/F3:TEL-JAK2
HTLV-1 infected T cells (MT-1, MT-2) 		0.033
0.025
- 		Gozgit et al. 2008
Yang et al. 2010
24 CMP6
(JAK1, JAK3, TYK2) 		pyridone tetracycle 0.001 CTLL-2
B9
U266
KMS11 		0.052-0.1
0.25
-
- 		Thompson et al. 2002
Lucet et al. 2006
Pedranzini et al. 2006
25 "13" sulfonamide aminoindazole 0.078 - - Antonysamy et al. 2009
26 comp 9
(JAK3, ALK, cKIT, GCK) 		polycyclic azaindole 0.001 TF-1-GMCSF (IC50)
HT2-IL2 (IC50) 		0.27
1.53 		Wang et al. 2009
27 "15a" polycyclic azaindole 0.0008 TF-1-GMCSF (IC50) 0.16 Wang et al. 2010
28 "40"
(JAK3) 		aminopyrazolopyrimidine 0.0002 TF-1-GMCSF (IC50)
HT2-IL2 (IC50) 		0.16
3.2 		Ledeboer et al. 2009
29 "29"
(JAK1, JAK3) 		pyrrolotriazine aminopyrrazole 0.0018 SET-2 0.11 Harikrishnan et al. 2011
30 atiprimod
(JAK3) 		azaspirane - FDCP-EpoR,JAK2wt
FDCP-EpoR,JAK2V617F
SET-2 		0.69
0.42
0.53 		Hamasaki et al. 2005
Quintás-Cardama et al. 2011
31 G6 stilbenoid
(diaryleten) 		0.060 Ba/F3:EpoR,JAK2V617F
HEL 		-
4.0 		Kiss et al. 2009
Majumder et al. 2010
Kirabo et al. 2011
32 NVP-BSK805
(JAK1, TYK2, ABL) 		diarylquinoxaline 0.00048
0.00058
0.00056 		Ba/F3:JAK2V617F
SET-2
MB-02
UKE-1
MUTZ-8 		0.039
0.051
0.064
0.071
0.331 		Baffert et al. 2010
33 "26"
(ABL) 		diarylquinoxaline 0.0073 SET-2 0.088 Pissot-Soldermann et al. 2010
34 hexabromo cyclohexane cyclohexane low µM γ-2A - Sandberg et al. 2005
35 XL019
(JAK1, JAK3, FLT3, PDGFRB, cKIT) 		arylaminopyrimidine 0.002 HEL - Paquette et al. 2008
Shah et al. 2008
Forsyth et al. 2012
36 CEP33779
(JAK1, JAK3) 		triazolopyridine 0.0018 irf1-bla TF-1 (IC50) 0.061 Dugan et al. 2012
37 "29"
(JAK1, JAK3, TYK2) 		triazolopyridine 0.0017 SET-2 (IC50) 0.212 Siu et al. 2013
38 "6"
(JAK1, JAK3, TYK2) 		imidazopyrrolopyridine 0.0021 TF-1-EPO (IC50) 0.097 Zak et al. 2012
39 "7"
(JAK1, JAK3, TYK2) 		imidazopyrrolopyridine 0.0012 TF-1-EPO (IC50) 0.86 Kulagowski et al. 2012
40 "31"
(JAK1, JAK3, TYK2) 		imidazopyrrolopyridine 0.068 TF-1-EPO (IC50) 7.68 Zak et al. 2013
41 "46"
(JAK1, TYK2) 		pyridine amide 0.028 TF-1-EPO (IC50) 1.7 Liang et al. 2013
42 "7j"
(JAK1, JAK3, TYK2) 		pyrazolopyrimidine 0.0001 SET-2 (IC50)
TF-1-EPO (IC50) 		0.0039
0.0074 		Hanan et al. 2012
43 "6"
(JAK3) 		pyrazolopyrimidine amine 0.003 Ba/F3:TEL-JAK2
SET-2
UKE1 		0.006
0.078
0.050 		Guan et al. 2013
44 "19a"
(JAK1, JAK3, CK2α2, KDR, ABL, FGR, TRKA, FLT4, FLT3, RET, ALK, FGFR1, AuroraA, LIMK1) 		methylimidazole 0.002 Ba/F3:TEL-JAK2
SET-2
UKE1 		0.012
0.014
0.055 		Su et al. 2014
45 NS-018
(JAK1, JAK3, TYK2, SRC, FYN, YES, LYNa, FGR, LCK, HCK, ABL, FLT3) 		pyrazinopyridine diamine 0.00072 Ba/F3:JAK2V617F
Ba/F3:TEL-JAK2
Ba/F3:MPLW515L
SET-2
Ba/F3:TEL-JAK3
MV4-11(FLT3-ITD) 		0.060 0.011 0.061 0.120 0.800 0.730 Nakaya et al. 2011
Nakaya et al. 2014
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