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首页-小分子抑制剂&激动剂-JAK/STAT Signaling-JAK-TG101209
TG101209

Chemical Structure : TG101209

CAS No.: 936091-14-4

TG101209 (SAR-317461, SAR317461, TG-101209)

货号: PC-42570Not For Human Use, Lab Use Only.

TG101209 (SAR-317461) is a potent, selective, orally bioavailable JAK2 inhibitor with IC50 of 6 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

TG101209 (SAR-317461) is a potent, selective, orally bioavailable JAK2 inhibitor with IC50 of 6 nM.
TG101209 also inhibits FLT3 (IC50=25 nM) and RET (IC50=17 nM) kinases, weakly inhibits JAK3 (IC50=168 nM).
TG101209 inhibits growth of Ba/F3 cells expressing JAK2V617F or MPLW515L mutations with IC50 of 200 nM, induces cell cycle arrest and apoptosis, and inhibits phosphorylation of JAK2V617F, STAT5 and STAT3.
TG101209 attenuates myelofibrosis in murine model of JAK2V617F-induced polycythemia vera.
TG101209 also potently inhibits BRD4 with Kd of 123 nM.

物理化学性质&存储条件

分子量 509.6668
分子式 C26H35N7O2S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Benzenesulfonamide, N-(1,1-dimethylethyl)-3-[[5-methyl-2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]amino]-

参考文献

1. Pardanani A, et al. Leukemia. 2007 Aug;21(8):1658-68.

2. Libani IV, et al. Blood. 2008 Aug 1;112(3):875-85.

3. Ciceri P, et al. Nat Chem Biol. 2014 Apr;10(4):305-12.

4. Wang Y, et al. Blood. 2009 Dec 3;114(24):5024-33.

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