|N-(1,1-二甲基乙基)-3-[[5-甲基-2-[[4-(4-甲基-1-哌嗪)苯基]氨基]-4-嘧啶]氨基]苯磺酰胺|CsnPharm

CAS No.: 936091-14-4

TG101209 Catalog No. CSN12694

Synonyms: TG 101209

TG 101209 is a potent and selective JAK2 inhibitor with IC50 of 6 nM, also inhibits Flt3 and RET with IC50 values of 25 nM and 17 nM, respectively.

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400-920-2911

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tech@csnpharm.cn

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技术信息

生物活性

描述Janus kinase 2 (JAK2) is a tyrosine kinase associated with the pathogenesis of myeloproliferative disorders. TG 101209 is a potent, orally bioavailable, small-molecule JAK2 inhibitor with an IC50 value of 6nM. It exhibits 28-fold potency for JAK2 relative to JAK3 in vitro. TG 101209 also shows inhibitory activities against FLT3 and RET with IC50 values of 25 and 17nM, respectively. TG 101209 inhibited the growth of Ba/F3-V617F and Ba/F3-W515L cells with IC50 values of 170 and 220 nM, respectively, but only had minimal effect on CTLL-2 cell growth with an IC50 value of 3400nM. In HEL cells homozygous for the JAK2V617F allele, treatment with TG 101209 at 4.6-38400nM resulted in a concentration-dependent inhibition of cell growth with an IC50 value of 152nM. TG 101209 also potently inhibited the proliferation of CHRF-288-11 cells with an IC50 value of 16nM. HEL cells treated with 600nM TG 101209 showed an increased percentage of Annexin V-positive cells compared to the background level at 24, 48, and 72h. Treatment of HEL cells with 1200nM TG 101209 for 24h increased the percentage of G0/G1 fraction cells compared with the background level. TG 101209 inhibited STAT5 phosphorylation in Ba/F3-V617F cells with an IC50 value of ~300nM. In a mouse model of JAK2V617F-induced hematopoietic disease, oral administration of TG 101209 (100mg/kg, b.i.d) for 10 days significantly prolonged the survival of animals compared with the vehicle-treated group^[3].
作用机制TG 101209 is a potent, selective JAK2 inhibitor. It docked and minimized in the ATP pocket of JAK2. TG 101209 effectively inhibited JAK2V617F and MPLW515L/K tyrosine kinases both in vitro and in vivo^[3].
参考文献

[1] Ma AC, Fan A, et al. A novel zebrafish jak2a(V581F) model shared features of human JAK2(V617F) polycythemia vera. Exp Hematol. 2009 Dec;37(12):1379-1386.e4.
[2] Pardanani A, Hood J, et al. TG101209, a small molecule JAK2-selective kinase inhibitor potently inhibits myeloproliferative disorder-associated JAK2V617F and MPLW515L/K mutations. Leukemia. 2007 Aug;21(8):1658-68.
[3] Pardanani A, Hood J, Lasho T, et al. TG101209, a small molecule JAK2-selective kinase inhibitor potently inhibits myeloproliferative disorder-associated JAK2V617F and MPLW515L/K mutations. Leukemia. 2007;21(8):1658-1668. doi:10.1038/sj.leu.2404750

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.9621 mL
- 9.8103 mL
- 19.6207 mL
- 5 mM
- 0.3924 mL
- 1.9621 mL
- 3.9241 mL
- 10 mM
- 0.1962 mL
- 0.9810 mL
- 1.9621 mL

技术信息

CAS号

936091-14-4

储存条件

粉末: Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C26H35N7O2S

运输

蓝冰

分子量

509.67

别名

TG 101209

溶解度

DMSO	230.0 mg/mL (451.3 mM) warming
Water	insoluble

动物实验配方

IP	2% DMSO+2% Tween80+30% PEG300+water	4.6 mg/mL	clear
PO	0.5% CMC-Na	52 mg/mL	suspension

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