Z BioInf
(→Charakterystyka wybranych niskocząsteczkowych inhibitorów domeny kinazowej JAK2) |
(→Charakterystyka wybranych niskocząsteczkowych inhibitorów domeny kinazowej JAK2) |
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| 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 | + | |[Shide et al. 2009]<br>[Shide et al. 2011] |
|- | |- | ||
|11 | |11 | ||
| Linia 99: | Linia 99: | ||
|<nowiki>-</nowiki> | |<nowiki>-</nowiki> | ||
|<nowiki>-</nowiki> | |<nowiki>-</nowiki> | ||
| − | |Verstovsek et al. 2008<br>Verstovsek et al. 2010<br>Mesa 2010 | + | |[Verstovsek et al. 2008]<br>[Verstovsek et al. 2010]<br>[Mesa 2010] |
|- | |- | ||
|12 | |12 | ||
| Linia 107: | Linia 107: | ||
|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 | |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 | |0.177<br>0.406<br>0.600<br>0.168<br>0.046<br>0.573 | ||
| − | |Koppikar et al. 2010 | + | |[Koppikar et al. 2010] |
|- | |- | ||
|13 | |13 | ||
| Linia 115: | Linia 115: | ||
|FDCP-EpoR,JAK2<sup>wt</sup><br>FDCP-EpoR,JAK2<sup>V617F</sup> | |FDCP-EpoR,JAK2<sup>wt</sup><br>FDCP-EpoR,JAK2<sup>V617F</sup> | ||
|2.1<br>0.25 | |2.1<br>0.25 | ||
| − | |Changelian et al. 2003<br>Chen et al. 2006<br>Clark et al. 2007<br>Manshouri et al. 2008<br>Meyer et al. 2010<br>Thoma et al. 2011 | + | |[Changelian et al. 2003]<br>[Chen et al. 2006]<br>[Clark et al. 2007]<br>[Manshouri et al. 2008]<br>[Meyer et al. 2010]<br>[Thoma et al. 2011] |
|- | |- | ||
|14 | |14 | ||
| Linia 123: | Linia 123: | ||
|Ba/F3:TEL-JAK2<br>SET-2<br>UKE1<br>HEL | |Ba/F3:TEL-JAK2<br>SET-2<br>UKE1<br>HEL | ||
|0.06<br>0.016<br>0.054<br>0.39 | |0.06<br>0.016<br>0.054<br>0.39 | ||
| − | |Hedvat et al. 2009<br>Ioannidis et al. 2011 | + | |[Hedvat et al. 2009]<br>[Ioannidis et al. 2011] |
|- | |- | ||
|15 | |15 | ||
| Linia 131: | Linia 131: | ||
|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 | |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 | |0.5<br>1.5<br>1.5<br>1.25<br>0.75<br>0.001<br>0.724 | ||
| − | |Pardanani et al. 2009<br>Tyner et al. 2010 | + | |[Pardanani et al. 2009]<br>[Tyner et al. 2010] |
|- | |- | ||
|16 | |16 | ||
| Linia 139: | Linia 139: | ||
|FDCP-EpoR,JAK2<sup>wt</sup><br>FDCP-EpoR,JAK2<sup>V617F</sup><br>HEL<br>SET-2<br>UKE-1 | |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 | |0.074<br>0.110<br>0.441<br>0.055<br>0.089 | ||
| − | |Olsen et al. 2008<br>Riaz Ahmed et al. 2011 | + | |[Olsen et al. 2008]<br>[Riaz Ahmed et al. 2011] |
|- | |- | ||
|17 | |17 | ||
| Linia 147: | Linia 147: | ||
|Ba/F3:JAK2<sup>V617F</sup><br>HEL<br>SET-2<br>Karpas-1106P<br>U266 | |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 | |0.16<br>1.726<br>0.217<br>0.348<br>1.350 | ||
| − | |Hart et al. 2011<br>William et al. 2011 | + | |[Hart et al. 2011]<br>[William et al. 2011] |
|- | |- | ||
|18 | |18 | ||
| Linia 155: | Linia 155: | ||
|HEL | |HEL | ||
|<nowiki>-</nowiki> | |<nowiki>-</nowiki> | ||
| − | |Sayyah et al. 2008 | + | |[Sayyah et al. 2008] |
|- | |- | ||
|19 | |19 | ||
| Linia 163: | Linia 163: | ||
|Ba/F3:TEL-JAK2 (IC<sub>50</sub>) | |Ba/F3:TEL-JAK2 (IC<sub>50</sub>) | ||
|1.62 | |1.62 | ||
| − | |Schenkel et al. 2011 | + | |[Schenkel et al. 2011] |
|- | |- | ||
|20 | |20 | ||
| Linia 171: | Linia 171: | ||
|irf1-bla HEL (IC<sub>50</sub>) | |irf1-bla HEL (IC<sub>50</sub>) | ||
|0.025 | |0.025 | ||
| − | |Lim et al. 2011 | + | |[Lim et al. 2011] |
|- | |- | ||
|21 | |21 | ||
| Linia 179: | Linia 179: | ||
|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>) | |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 | |0.110<br>0.057<br>0.016<br>0.017<br>0.040<br>0.026 | ||
| − | |Howard et al. 2009<br>Dawson et al. 2010 | + | |[Howard et al. 2009]<br>[Dawson et al. 2010] |
|- | |- | ||
|22 | |22 | ||
Wersja z 21:59, 17 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 |