Z BioInf
Skocz do: nawigacja, szukaj
(→‎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]
Źródło: „https://bioinfo.imdik.pan.pl/mediawiki/index.php?title=JAK2_inhibitor&oldid=1311”