|N-(叔丁基)-3-((5-甲基-2-((4-(2-吡咯烷-1-基)乙氧基)苯基)氨基)嘧啶-4-基)氨基)苯磺酰胺二盐酸盐水合物|CsnPharm

CAS No.: 1374744-69-0

N-(tert-Butyl)-3-((5-methyl-2-((4-(2-(pyrrolidin-1-yl)ethoxy)phenyl)amino)pyrimidin-4-yl)amino)benzenesulfonamide dihydrochloride hydrate Catalog No. CSN27527

Synonyms: TG-101348 hydrochloride hydrate;SAR 302503 hydrochloride hydrate;Fedratinib dihydrochloride hydrate

Fedratinib hydrochloride hydrate (TG-101348 hydrochloride hydrate) is a potent, selective, ATP-competitive and orally active JAK2 inhibitor with IC50s of 3 nM for both JAK2 and JAK2V617F kinase. Fedratinib hydrochloride hydrate shows 35- and 334-fold selectivity over JAK1 and JAK3, respectively. Fedratinib hydrochloride hydrate induces cancer cell apoptosis and has the potential for myeloproliferative disorders research.

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

描述The JAK2V617F mutation is present in the majority of cases of myeloproliferative disease (MPD), including polycythemia vera (PV), essential thrombocythemia (ET), and primary myelofibrosis (PMF), and is an attractive candidate for molecularly targeted therapy. Fedratinib hydrochloride hydrate is a potent, selective and ATP-competitive JAK2 inhibitor with IC₅₀s of 3 nM for both JAK2 and JAK2V617F kinase. Fedratinib inhibited proliferation of a human erythroblast leukemia (HEL) cell line that harbors the JAK2V617F mutation, as well as a murine pro-B cell line expressing human JAK2V617F (Ba/F3 JAK2V617F), with an IC₅₀ value of approximately 300 nM for either line. Proliferation of parental Ba/F3 cells was inhibited to a comparable level, with an IC₅₀ value of ~420 nM. Furthermore, exposure of these cells to fedratinib (0.1, 0.3, 1, 3, and 10 μM) reduced STAT5 phosphorylation at concentrations that parallel the concentrations required to inhibit cell proliferation. Moreover, fedratinib (0.1, 0.3, 1, 3, and 10 μM) induced apoptosis in both HEL and Ba/F3 JAK2V617F cells in a dose-dependent manner. In vivo, fedratinib (60-120 mg/kg; oral gavage; twice daily; for 42 days) caused a dose-dependent reduction in polycythemia and splenomegaly of treated C57Bl/6 mice^[1].
参考文献

[1] Wernig G, Kharas MG, Okabe R, et al. Efficacy of TG101348, a selective JAK2 inhibitor, in treatment of a murine model of JAK2V617F-induced polycythemia vera. Cancer Cell. 2008 Apr;13(4):311-20.
[2] Geron I, et al. Selective inhibition of JAK2-driven erythroid differentiation of polycythemia vera progenitors. Cancer Cell. 2008 Apr;13(4):321-30.

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
- 1.6244 mL
- 8.1220 mL
- 16.2439 mL
- 5 mM
- 0.3249 mL
- 1.6244 mL
- 3.2488 mL
- 10 mM
- 0.1624 mL
- 0.8122 mL
- 1.6244 mL

技术信息

CAS号

1374744-69-0

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C27H40Cl2N6O4S

运输

蓝冰

分子量

615.62

别名

TG-101348 hydrochloride hydrate;SAR 302503 hydrochloride hydrate;Fedratinib dihydrochloride hydrate;SAR-302503;TG-101348

溶解度

DMSO	240.0 mg/mL (389.9 mM) warming

动物实验配方

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

N-(tert-Butyl)-3-((5-methyl-2-((4-(2-(pyrrolidin-1-yl)ethoxy)phenyl)amino)pyrimidin-4-yl)amino)benzenesulfonamide dihydrochloride hydrate Catalog No. CSN27527

靶点选择性

请登录您的专属账户

确认信息