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CX-6258 hydrochloride (Pim-Kinase Inhibitor X) 是一种强效选择性的泛 Pim 激酶抑制剂,对Pim-1、Pim-2 和 Pim-3 作用的IC50值分别为 5、25 和 16 nM。
CX-6258 hydrochloride (Pim-Kinase Inhibitor X) 是一种强效选择性的泛 Pim 激酶抑制剂,对Pim-1、Pim-2 和 Pim-3 作用的IC50值分别为 5、25 和 16 nM。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 248 | 现货 | |
5 mg | ¥ 579 | 现货 | |
10 mg | ¥ 928 | 现货 | |
25 mg | ¥ 1,850 | 现货 | |
50 mg | ¥ 2,970 | 现货 | |
100 mg | ¥ 4,290 | 现货 | |
200 mg | ¥ 5,950 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 635 | 现货 |
产品描述 | CX-6258 hydrochloride (Pim-Kinase Inhibitor X) is an effective, orally efficacious Pim1/2/3 kinase inhibitor (IC50: 5/25/16 nM). |
靶点活性 | Pim1:5 nM, Pim2:25 nM, Pim3:16 nM |
体外活性 | CX-6258 对一系列人类癌症细胞系展现出抗增殖活性(IC50:0.02-3.7 μM),尤其对急性白血病细胞系更为敏感。CX-6258 结合多柔比星(摩尔比 10:1)以及与紫杉醇(摩尔比 100:1)联用,能产生协同杀伤细胞的效果(CI50:0.4 和 0.56)。 |
体内活性 | 在携带MV-4-11异种移植瘤的小鼠中,CX-6258以剂量依赖的方式抑制肿瘤生长,其中50/100 mg/kg的剂量能够产生45%/75%的肿瘤生长抑制效果。 |
激酶实验 | Pim-1 and Pim-2 inhibitions are measured in radiometric assays using human recombinant Pim-1 at [ATP] = 30 μM (substrate RSRHSSYPAGT) and human recombinant Pim-2 at [ATP] = 5 μM (substrate RSRHSSYPAGT). The radiometric assay for Pim-3 uses RSRHSSYPAGT as a substrate in the presence of [ATP] = 155 μM. |
别名 | CX-6258 HCl, Pim-Kinase Inhibitor X |
分子量 | 498.4 |
分子式 | C26H24ClN3O3·HCl |
CAS No. | 1353859-00-3 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
溶解度信息 | H2O: 82 mg/mL (164.5 mM) DMSO: 53 mg/mL (106.3 mM) Ethanol: 1 mg/mL (2.0 mM), Heating is recommended. | ||||||||||||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||||||||||||
Ethanol/DMSO/H2O
DMSO/H2O
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