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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  | In stock | |
| 5 mg | ¥ 579  | In stock | |
| 10 mg | ¥ 928  | In stock | |
| 25 mg | ¥ 1,850  | In stock | |
| 50 mg | ¥ 2,970  | In stock | |
| 100 mg | ¥ 4,290  | In stock | |
| 200 mg | ¥ 5,950  | In stock | |
| 1 mL x 10 mM (in DMSO) | ¥ 635  | In stock | 
CX-6258 hydrochloride 相关产品
| 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 |  Pim2:25 nM, Pim1:5 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 | Pim-Kinase Inhibitor X, CX-6258 HCl | 
| 分子量 | 498.4 | 
| 分子式 | C26H24ClN3O3·HCl | 
| CAS No. | 1353859-00-3 | 
| Smiles | Cl.CN1CCCN(CC1)C(=O)c1cccc(c1)-c1ccc(\C=C2\C(=O)Nc3ccc(Cl)cc23)o1 | 
| 密度 | no data available | 
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||||||||||||
| 溶解度信息 | H2O: 82 mg/mL (164.53 mM), Sonication is recommended.  DMSO: 53 mg/mL (106.34 mM), Sonication is recommended.  Ethanol: 1 mg/mL (2.0 mM), Heating is recommended.   | ||||||||||||||||||||||||||||||||||||||||
| 体内实验配方 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.01 mM), Sonication is recommended.  请按顺序添加溶剂,在添加下一种溶剂之前,尽可能使溶液澄清。如有必要,可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考,体内配方并不是绝对的,请根据不同情况进行调整。 | ||||||||||||||||||||||||||||||||||||||||
溶液配制表  | |||||||||||||||||||||||||||||||||||||||||
Ethanol/DMSO/H2O 
 DMSO/H2O 
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