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CAS No.: 1092499-93-8

NVP-BSK805 Catalog No. CSN17137

Synonyms: BSK 805

NVP-BSK805 is a selective JAK2 and JAK2(V617F) mutant inhibitor with IC50 value of 0.48 nM, with >20-fold selectivity over TYK2, JAK3 and JAK1 (IC50 values of 10.8, 18.7 and 31.6 nM, respectively).

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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

靶点 JAK2

IC50:0.5nM
描述NVP-BSK805 is a selective JAK2 inhibitor with IC50 value of 7.3nM, much selective to JAK2 over JAK1 (IC50=303nM), JAK3 (IC50=610nM) and TYK2 (IC50=384nM) . For NVP-BSK805 inhibited both JAK2 and JAK2^V617F facilitated its potency against cell lines bearing JAK2^V617F, including Ba/F3 JAK2^V617F, SET-2 JAK2^V617F, MB-02 JAK2^V617F, UKE-1 JAK2^V617F and MUTZ-8 JAK2^V617F with GI50 values of 39, 51, 64, 71 and 331nM, respectively, as well as blunted constitutive STAT5 phosphorylation in JAK2^V617F-bearing SET-2 cells at concentration>100nM post 1-hour treatment. A time- and concentration-dependent induction of apoptosis shown by increased level of cleaved PARP and decreased Bcl-xL could be observed in JAK2^V617F-bearing SET-2 cells treated with NVP-BSK805 at concentration of 150nM or 1μM post 24h or 48h. NVP-BSK805 also possesses pharmacodynamics in vivo. Oral administration of 150mg/kg led significant reduction of phosphorylated STAT5 in spleens of SCID beige mice bearing Ba/F3 JAK2^V617F cells post 12h. A reduction of Ba/F3 JAK2^V617F cell leukemic burden and spleen weight was detected post 5-day treatment. Also, NVP-BSK805 at dose of 100mg/kg potently suppressed recombinant human erythropoietin-induced polycythemia and extramedullary erythropoiesis in mice and rats.
作用机制NVP-BSK805 acts in an ATP-competitive manner.^[1]^[2]
动物研究
剂量
Mice: 90 mg/kg^[3] (i.v.); 150 mg/kg^[1] (p.o.)

给药途径
i.v., p.o.
参考文献

动物研究
剂量	Mice: 90 mg/kg^[3] (i.v.); 150 mg/kg^[1] (p.o.)
给药途径	i.v., p.o.

[1] Baffert F, Régnier CH, et al. Potent and selective inhibition of polycythemia by the quinoxaline JAK2 inhibitor NVP-BSK805. Mol Cancer Ther. 2010 Jul;9(7):1945-55.
[2] Baffert F, Régnier CH, et al. Potent and selective inhibition of polycythemia by the quinoxaline JAK2 inhibitor NVP-BSK805. Mol Cancer Ther. 2010 Jul;9(7):1945-55.

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
- 2.0385 mL
- 10.1927 mL
- 20.3854 mL
- 5 mM
- 0.4077 mL
- 2.0385 mL
- 4.0771 mL
- 10 mM
- 0.2039 mL
- 1.0193 mL
- 2.0385 mL

技术信息

CAS号

1092499-93-8

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

C27H28F2N6O

运输

蓝冰

分子量

490.55

别名

BSK 805

溶解度

DMSO	95.0 mg/mL (193.7 mM)
Water	100.0 mg/mL (203.9 mM)

动物实验配方

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NVP-BSK805 Catalog No. CSN17137

靶点选择性

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