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Fedratinib hydrochloride hydrate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Fedratinib hydrochloride hydrate图片
规格:98%
分子量:615.62
包装与价格:
包装价格(元)
5mg电议
10mg电议
100mg电议
200mg电议
500mg电议
1g电议
2g电议
5g电议

产品介绍
Fedratinibhydrochloridehydrate(TG-101348hydrochloridehydrate)是一种有效的,选择性的,ATP竞争性和具有口服活性的JAK2抑制剂,对于JAK2和JAK2V617F激酶的IC50均为3nM。Fedratinibhydrochloridehydrate对JAK2的选择性分别比JAK1和JAK3高35倍和334倍。Fedratinibhydrochloridehydrate可诱导癌细胞凋亡(apoptosis),并可用于骨髓增生性疾病的研究。
货号:ajcx29334
CAS:1374744-69-0
分子式:C27H40Cl2N6O4S
分子量:615.62
溶解度:DMSO: 250 mg/mL (406.09 mM)
纯度:98%
存储:Store at -20°C
库存:现货

Background:

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[1][2].

Fedratinib (TG101348) inhibits 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[1]. Exposure of these cells to Fedratinib (TG101348) (0.1 μM, 0.3 μM, 1 μM, 3 μM, and 10 μM) reduces STAT5 phosphorylation at concentrations that parallel the concentrations required to inhibit cell proliferation[1]. Fedratinib (TG101348) (0.1 μM, 0.3 μM, 1 μM, 3 μM, and 10 μM) induces apoptosis in both HEL and Ba/F3 JAK2V617F cells in a dose-dependent manner[1].

Fedratinib (TG101348; 60-120 mg/kg; oral gavage; twice daily; for 42 days; C57Bl/6 mice) trewatment shows a dose-dependent reduction in polycythemia and a marked dose-dependent reduction in splenomegaly of treated animals[1]. Animal Model: C57Bl/6 mice induced by the JAK2V617F mutation[1]

[1]. Wernig G, 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.