Z BioInf
(→Charakterystyka wybranych niskocząsteczkowych inhibitorów domeny kinazowej JAK2) |
(→Charakterystyka wybranych niskocząsteczkowych inhibitorów domeny kinazowej JAK2) |
||
Linia 91: | Linia 91: | ||
|Ba/F3:JAK2<sup>V617F</sup> | |Ba/F3:JAK2<sup>V617F</sup> | ||
|0.13-0.20 | |0.13-0.20 | ||
− | |[Shide et al. 2009]<br>[Shide et al. 2011] | + | |[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 | |11 | ||
Linia 187: | Linia 187: | ||
|SET-2 (JAK2<sup>V617F/wt</sup>)<br>Ba/F3:TEL-JAK2<br>HTLV-1 infected T cells (MT-1, MT-2) | |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>- | |0.033<br>0.025<br>- | ||
− | |Gozgit et al. 2008<br>Yang et al. 2010 | + | |[Gozgit et al. 2008]<br>[Yang et al. 2010] |
|- | |- | ||
|23 | |23 | ||
Linia 195: | Linia 195: | ||
|CTLL-2<br>B9<br>U266<br>KMS11 | |CTLL-2<br>B9<br>U266<br>KMS11 | ||
|0.052-0.1<br>0.25<br>-<br>- | |0.052-0.1<br>0.25<br>-<br>- | ||
− | |Thompson et al. 2002<br>Lucet et al. 2006<br>Pedranzini et al. 2008 | + | |[Thompson et al. 2002]<br>[Lucet et al. 2006]<br>[Pedranzini et al. 2008] |
|- | |- | ||
|24 | |24 | ||
Linia 203: | Linia 203: | ||
|<nowiki>-</nowiki> | |<nowiki>-</nowiki> | ||
|<nowiki>-</nowiki> | |<nowiki>-</nowiki> | ||
− | |Antonysamy et al. 2009 | + | |[Antonysamy et al. 2009] |
|- | |- | ||
|25 | |25 | ||
Linia 211: | Linia 211: | ||
|TF-1-GMCSF (IC<sub>50</sub>)<br>HT2-IL2 (IC<sub>50</sub>) | |TF-1-GMCSF (IC<sub>50</sub>)<br>HT2-IL2 (IC<sub>50</sub>) | ||
|0.27<br>1.53 | |0.27<br>1.53 | ||
− | |Wang et al. 2009 | + | |[Wang et al. 2009] |
|- | |- | ||
|26 | |26 | ||
Linia 219: | Linia 219: | ||
|TF-1-GMCSF (IC<sub>50</sub>) | |TF-1-GMCSF (IC<sub>50</sub>) | ||
|0.16 | |0.16 | ||
− | |Wang et al. 2010 | + | |[Wang et al. 2010] |
|- | |- | ||
|27 | |27 | ||
Linia 227: | Linia 227: | ||
|TF-1-GMCSF (IC<sub>50</sub>)<br>HT2-IL2 (IC<sub>50</sub>) | |TF-1-GMCSF (IC<sub>50</sub>)<br>HT2-IL2 (IC<sub>50</sub>) | ||
|0.16<br>3.2 | |0.16<br>3.2 | ||
− | |Ledeboer et al. 2009 | + | |[Ledeboer et al. 2009] |
|- | |- | ||
|28 | |28 | ||
Linia 235: | Linia 235: | ||
|SET-2 | |SET-2 | ||
|0.11 | |0.11 | ||
− | |Harikrishnan et al. 2011 | + | |[Harikrishnan et al. 2011] |
|- | |- | ||
|29 | |29 | ||
Linia 243: | Linia 243: | ||
|FDCP-EpoR,JAK2<sup>wt</sup><br>FDCP-EpoR,JAK2<sup>V617F</sup><br>SET-2 | |FDCP-EpoR,JAK2<sup>wt</sup><br>FDCP-EpoR,JAK2<sup>V617F</sup><br>SET-2 | ||
|0.69<br>0.42<br>0.53 | |0.69<br>0.42<br>0.53 | ||
− | |Hamasaki et al. 2005<br>Quintás-Cardama et al. 2011 | + | |[Hamasaki et al. 2005]<br>[Quintás-Cardama et al. 2011] |
|- | |- | ||
|30 | |30 | ||
Linia 251: | Linia 251: | ||
|Ba/F3:EpoR,JAK2<sup>V617F</sup><br>HEL | |Ba/F3:EpoR,JAK2<sup>V617F</sup><br>HEL | ||
|<nowiki>-</nowiki><br>4.0 | |<nowiki>-</nowiki><br>4.0 | ||
− | |Kiss et al. 2009<br>Majumder et al. 2010<br>Kirabo et al. 2011 | + | |[Kiss et al. 2009]<br>[Majumder et al. 2010]<br>[Kirabo et al. 2011] |
|- | |- | ||
|31 | |31 | ||
Linia 259: | Linia 259: | ||
|Ba/F3:JAK2<sup>V617F</sup><br>SET-2<br>MB-02<br>UKE-1<br>MUTZ-8 | |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 | |0.039<br>0.051<br>0.064<br>0.071<br>0.331 | ||
− | |Baffert et al. 2010 | + | |[Baffert et al. 2010] |
|- | |- | ||
|32 | |32 | ||
Linia 267: | Linia 267: | ||
|SET-2 | |SET-2 | ||
|0.088 | |0.088 | ||
− | |Pissot-Soldermann et al. 2010 | + | |[Pissot-Soldermann et al. 2010] |
|- | |- | ||
|33 | |33 | ||
Linia 275: | Linia 275: | ||
|g-2A | |g-2A | ||
|<nowiki>-</nowiki> | |<nowiki>-</nowiki> | ||
− | |Sandberg et al. 2005 | + | |[Sandberg et al. 2005] |
|- | |- | ||
|34 | |34 | ||
Linia 283: | Linia 283: | ||
|HEL | |HEL | ||
|<nowiki>-</nowiki> | |<nowiki>-</nowiki> | ||
− | |Paquette et al. 2008<br>Shah et al. 2008<br>Forsyth et al. 2012 | + | |[Paquette et al. 2008]<br>[Shah et al. 2008]<br>[Forsyth et al. 2012] |
|- | |- | ||
|35 | |35 | ||
Linia 291: | Linia 291: | ||
|irf1-bla TF-1 (IC<sub>50</sub>) | |irf1-bla TF-1 (IC<sub>50</sub>) | ||
|0.061 | |0.061 | ||
− | |Dugan et al. 2012 | + | |[Dugan et al. 2012] |
|- | |- | ||
|36 | |36 | ||
Linia 299: | Linia 299: | ||
|SET-2 (IC<sub>50</sub>) | |SET-2 (IC<sub>50</sub>) | ||
|0.212 | |0.212 | ||
− | |Siu et al. 2013 | + | |[Siu et al. 2013] |
|- | |- | ||
|37 | |37 | ||
Linia 307: | Linia 307: | ||
|TF-1-EPO (IC<sub>50</sub>) | |TF-1-EPO (IC<sub>50</sub>) | ||
|0.097 | |0.097 | ||
− | |Zak et al. 2012 | + | |[Zak et al. 2012] |
|- | |- | ||
|38 | |38 | ||
Linia 315: | Linia 315: | ||
|TF-1-EPO (IC<sub>50</sub>) | |TF-1-EPO (IC<sub>50</sub>) | ||
|0.86 | |0.86 | ||
− | |Kulagowski et al. 2012 | + | |[Kulagowski et al. 2012] |
|- | |- | ||
|39 | |39 | ||
Linia 323: | Linia 323: | ||
|TF-1-EPO (IC<sub>50</sub>) | |TF-1-EPO (IC<sub>50</sub>) | ||
|7.68 | |7.68 | ||
− | |Zak et al. 2013 | + | |[Zak et al. 2013] |
|- | |- | ||
|40 | |40 | ||
Linia 331: | Linia 331: | ||
|TF-1-EPO (IC<sub>50</sub>) | |TF-1-EPO (IC<sub>50</sub>) | ||
|1.7 | |1.7 | ||
− | |Liang et al. 2013 | + | |[Liang et al. 2013] |
|- | |- | ||
|41 | |41 | ||
Linia 339: | Linia 339: | ||
|SET-2 (IC<sub>50</sub>)<br>TF-1-EPO (IC<sub>50</sub>) | |SET-2 (IC<sub>50</sub>)<br>TF-1-EPO (IC<sub>50</sub>) | ||
|0.0039<br>0.0074 | |0.0039<br>0.0074 | ||
− | |Hanan et al. 2012 | + | |[Hanan et al. 2012] |
|- | |- | ||
|42 | |42 | ||
Linia 347: | Linia 347: | ||
|Ba/F3:TEL-JAK2<br>SET-2<br>UKE1 | |Ba/F3:TEL-JAK2<br>SET-2<br>UKE1 | ||
|0.006<br>0.078<br>0.050 | |0.006<br>0.078<br>0.050 | ||
− | |Guan et al. 2013 | + | |[Guan et al. 2013] |
|- | |- | ||
|43 | |43 | ||
Linia 355: | Linia 355: | ||
|Ba/F3:TEL-JAK2<br>SET-2<br>UKE1 | |Ba/F3:TEL-JAK2<br>SET-2<br>UKE1 | ||
|0.012<br>0.014<br>0.055 | |0.012<br>0.014<br>0.055 | ||
− | |Su et al. 2014 | + | |[Su et al. 2014] |
|} | |} |
Wersja z 13:23, 19 maj 2014
Charakterystyka wybranych niskocząsteczkowych inhibitorów domeny kinazowej JAK2
Lp. | inhibitor (inne hamowane kinazy) |
klasa chemiczna | test enzym. | test komórkowy | literatura | |
---|---|---|---|---|---|---|
IC50 (µM) | linia komórkowa | 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 | - | - | [Verstovsek et al. 2008] [Verstovsek et al. 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 | 0.003 | 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, CaMKIIδ,γ, 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 | cyclohexane | low µM | 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, 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] |