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NVP-BSK805 Trihydrochloride

品牌
Sigma-Aldrich
CAS
2320258-95-3
货号
SML2628
规格纯度
≥98% (HPLC)
参考价格
1168.11 *本价格含增值税费
促销
服务
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  • 增值税票
数量
-+
产品名称:
2320258-95-3
NVP-BSK805 Trihydrochloride
8-[3,5-Difluoro-4-(4-morpholinylmethyl)phenyl]-2-[1-(4-piperidinyl)-1H-pyrazol-4-yl]quinoxaline trihydrochloride
NVP-BSK 805 3HCl
4-(2,6-Difluoro-4-(3-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)quinoxalin-5-yl)benzyl)morpholine trihydrochloride
8-(3,5-Difluoro-4-morpholin-4-ylmethyl-phenyl)-2-(1-piperidin-4-yl-1H-pyrazol-4-yl)-quinoxaline trihydrochloride
BSK805, 3HCl
BSK 805 3HCl
产品介绍:

产品说明

生化/生理作用

NVP-BSK805 is a selective, ATP-competitive (Ki = 0.43 nM) Janus kinase 2 (JAK2) inhibitor (IC50 = 0.58 and 0.56 nM against full-length wild-type and V617F JAK2, respectively) with greatly reduced potency against TYK2, JAK3, JAK1 (IC50 = 10.76, 18.68, 31.63 nM against respective JAK homology domain 1) and >300-fold selectivity over a panel of 36 other kinases. BSK805 potently inhibits STAT5 phosphorylation (by >90% at 100 nM; MB-02 & SET-2 cells) and proliferation in JAK2V617F mutant cultures in vitro (GI50= 39-331 nM; 75% SET-2 growth inhibition at 150 nM) and in Ba/F3 JAK2V617F-bearing mice in vivo (150 mg/kg p.o.). BSK805 daily oral administration is also efficacious against rhEpo-induced splenomegaly and polycythemia in mice (50-100 mg/kg) and rats (25-50 mg/kg) with good pharmacokinetics and oral avilability.

基本信息

经验(实验)分子式C27H28F2N6O·3HCl
分子量599.93
MDL编号MFCD22419018

产品性质

测定≥98% (HPLC)
形式powder
颜色faint yellow to dark orange
溶解性H2O: 2 mg/mL, clear
储存温度−20℃

安全信息

储存分类代码11 - Combustible Solids
WGKWGK 3
闪点(F)Not applicable
闪点(C)Not applicable

Sigma-Aldrich

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