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NVP-BSK805
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。
NVP-BSK805图片
CAS NO:1092499-93-8
包装:100 mg
市场价:9752元

产品名称
NVP-BSK805 2HCl
BSK 805
8-[3,5-二氟-4-(4-吗啉基甲基)苯基]-2-[1-(4-哌啶基)-1H-吡唑-4-基]喹喔啉
产品介绍
NVP-BSK805 是 ATP 竞争性的JAK2抑制剂,对 JAK1 JH1、 JAK2 JH1 (JAK 同源 1)、JAK3 JH1和 TYK2 JH1 的IC50值分别为 31.63、0.48、8.68 和 10.76 nM。

产品描述

NVP-BSK805 is an ATP-competitive JAK2 inhibitor.

体外活性

GI50 of<100 nM. NVP-BSK805 blocks the STAT5 phosphorylation at ≥100 nM concentrations, and shows a bias for JAK2 over JAK1 and JAK3 inhibition in the JAK2V617F-mutant cell lines. NVP-BSK805 (5 μM) improves P-gp inhibitory activity. NVP-BSK805 increases sensitization of drug-resistant KBV20C cancer cells to VIC treatment at 10 μM, and such an effect is more effective than a 5 μM dose.

体内活性

NVP-BSK805 (150 mg/kg, p.o.) blocks STAT5 phosphorylation, splenomegaly, and leukemic cell spreading in a Ba/F3 JAK2V617F cell-driven mouse model. NVP-BSK805 (50, 75, and 100 mg/kg, p.o.) also suppresses rhEpo-mediated polycythemia and splenomegaly in BALB/c mice.

Cas No.

1092499-93-8

分子式

C27H28F2N6O

分子量

490.559

别名

NVP-BSK805 2HCl;BSK 805;8-[3,5-二氟-4-(4-吗啉基甲基)苯基]-2-[1-(4-哌啶基)-1H-吡唑-4-基]喹喔啉

储存和溶解度

DMSO:10mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years