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NVP-BSK805 (BSK 805) 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。
NVP-BSK805 (BSK 805) 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。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
100 mg | ¥ 9,752 | 5日内发货 |
产品描述 | NVP-BSK805 (BSK 805) is an ATP-competitive JAK2 inhibitor. |
靶点活性 | JAK1 JH1:31.63 nM, FL JAK2 (V617F):0.56 nM, TYK2 JH1:10.76 nM, JAK2 JH1:0.48 nM, JAK3 JH1:18.68 nM, FL JAK2 (WT):0.58 nM |
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. |
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 |
分子量 | 490.55 |
分子式 | C27H28F2N6O |
CAS No. | 1092499-93-8 |
密度 | 1.4 g/cm3 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
溶解度信息 | DMSO: 10 mM | ||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||
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