购物车
- 全部删除
- 您的购物车当前为空
KPT9274 (PAK4-IN-1) 是一种非竞争性的 PAK4 和 NAMPT 双重抑制剂(IC50= ~120 nM)。它是一种口服生物可利用的小分子。
KPT9274 (PAK4-IN-1) 是一种非竞争性的 PAK4 和 NAMPT 双重抑制剂(IC50= ~120 nM)。它是一种口服生物可利用的小分子。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 579 | 现货 | |
2 mg | ¥ 866 | 现货 | |
5 mg | ¥ 1,490 | 现货 | |
10 mg | ¥ 2,380 | 现货 | |
25 mg | ¥ 3,980 | 现货 | |
50 mg | ¥ 5,720 | 现货 | |
100 mg | ¥ 7,780 | 现货 | |
500 mg | ¥ 15,600 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 1,960 | 现货 |
产品描述 | KPT9274 (PAK4-IN-1) is a non-competitive dual inhibitor of PAK4 and NAMPT(IC50= ~120 nM). It is an orally bioavailable small molecule. |
靶点活性 | NAMPT:~120 nM |
体外活性 | In several human RCC cell lines, KPT-9274 interferences with PAK4 and NAD biosynthetic pathways leading to reduction of G2/M transit as well as induction of apoptosis and decrease in cell invasion and migration. The inhibition of the PAK4 pathway by KPT-9274 attenuates nuclear β-catenin as well as the Wnt/β-catenin targets cyclin D1 and c-Myc. |
体内活性 | In mice, KPT-9274 (200 mg/kg) daily is administered either intravenously or orally with the absence of any signs of toxicity. |
细胞实验 | 786-0, ACHN, Caki-1 and U-2 OS cells are treated with KPT-9274 (1 μM and 5 μM) incubating for 12 hours. |
动物实验 | 786-O (VHL-mut) human RCC xenograft model (nude mice) is treated with KPT-9274 (100 and 200 mg/kg),prepared in 58% Polyvinylpyrrolidone K30 + 21% methyl cellulose + 21% Phospholipon 90 g, by oral gavage. |
别名 | PAK4-IN-1, KPT-9274, KPT 9274 |
分子量 | 610.62 |
分子式 | C35H29F3N4O3 |
CAS No. | 1643913-93-2 |
Smiles | Nc1ccc(\C=C\C(=O)NCc2cc3cc(cc(-c4ccc(F)cc4)c3o2)-c2ccc(cc2)C(=O)N2CCC(F)(F)CC2)cn1 |
密度 | 1.39 g/cm3 (Predicted) |
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: 55 mg/mL (90.07 mM) | ||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||
DMSO
|
版权所有©2015-2024 TargetMol Chemicals Inc.保留所有权利.
评论内容