Z BioInf
(→Charakterystyka wybranych niskocząsteczkowych inhibitorów domeny kinazowej JAK2) |
(→Charakterystyka wybranych niskocząsteczkowych inhibitorów domeny kinazowej JAK2) |
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| Linia 99: | Linia 99: | ||
|<nowiki>-</nowiki> | |<nowiki>-</nowiki> | ||
|<nowiki>-</nowiki> | |<nowiki>-</nowiki> | ||
| − | |[Verstovsek et al. 2008]<br>[Verstovsek et al. 2010]<br>[Mesa | + | |{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 | |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] | + | |[http://bloodjournal.hematologylibrary.org/content/115/14/2919.abstract 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] | + | |[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 | |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] | + | |[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 | |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] | + | |[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 | |16 | ||
!scope="row" style="background-color:LemonChiffon" |SGI1252<br>(JAK1, JAK3, TYK2, YES, FLT3, ABL, SRC, LCK) | !scope="row" style="background-color:LemonChiffon" |SGI1252<br>(JAK1, JAK3, TYK2, YES, FLT3, ABL, SRC, LCK) | ||
|diaminopyrimidine | |diaminopyrimidine | ||
| − | |0.002<br>0.0197 | + | |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 | |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] | + | |[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 | |17 | ||
Wersja z 18:01, 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 | - | - | {http://abstracts.hematologylibrary.org/cgi/content/abstract/ashmtg;110/11/3538 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 | 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] |