NVP-BSK805|cas:1092499-93-8|西域试剂

NVP-BSK805,99.76%

产品编号：Bellancom-14722| CAS NO：1092499-93-8| 分子式：C₂₇H₂₈F₂N₆O| 分子量：490.55

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货号	价格	库存与货期
Bellancom-14722	￥1600.00	杭州北京（现货）
Bellancom-14722	￥2600.00	杭州北京（现货）
Bellancom-14722	￥5200.00	杭州北京（现货）
Bellancom-14722	￥8300.00	杭州北京（现货）
Bellancom-14722	￥13300.00	杭州北京（现货）

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NVP-BSK805

产品介绍

NVP-BSK805 是一种 ATP 竞争性的 JAK2 抑制剂，对 JAK2 JH1 (JAK 同源 1)，JAK1 JH1，JAK3 JH1，和 TYK2 JH1 的 IC₅₀ 值分别为 0.48 nM，31.63 nM，18.68 nM 和 10.76 nM。

生物活性

NVP-BSK805 is an ATP-competitive JAK2 inhibitor, with IC₅₀s of 0.48 nM, 31.63 nM, 18.68 nM, and 10.76 nM for JAK2 JH1 (JAK homology 1), JAK1 JH1, JAK3 JH1, and TYK2 JH1, respectively.

体外研究

NVP-BSK805 (BSK 805) is a JAK2 inhibitor, with IC₅₀s of 0.48 nM, 31.63 nM, 18.68 nM, and 10.76 nM for JAK2 JH1 (JAK homology 1), JAK1 JH1, JAK3 JH1, and TYK2 JH1, respectively. NVP-BSK805 inhibits the full-length wild-type JAK2 (FL JAK2 wt) and FL JAK2 V617F activity, with IC₅₀s of 0.58 ± 0.03 and 0.56 ± 0.04 nM. NVP-BSK805 is ATP-competitive, with aclculated K_i of 0.43 ± 0.02 nM. NVP-BSK805 suppresses the growth of JAK2^V617F-bearing acute myeloid leukemia cell lines with 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 JAK2^V617F-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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

NVP-BSK805 (BSK 805; 150 mg/kg, p.o.) blocks STAT5 phosphorylation, splenomegaly, and leukemic cell spreading in a Ba/F3 JAK2^V617F 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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

性状

Solid

溶解性数据

In Vitro:

DMSO : 125 mg/mL (254.82 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0385 mL	10.1926 mL	20.3853 mL
5 mM	0.4077 mL	2.0385 mL	4.0771 mL
10 mM	0.2039 mL	1.0193 mL	2.0385 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式