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CX-6258
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CX-6258图片
CAS NO:1202916-90-2
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
CX 6258
产品介绍
CX6258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。

产品描述

CX-6258 is an orally valid Pim 1/2/3 kinase(IC50=5 nM/25 nM/16 nM) inhibitor. It has good biological activity and kinase specificity.

体外活性

CX-6258 shows antiproliferative activity against a panel of human cancer cell lines with IC50 of 0.02-3.7 μM, mostly sensitive to acute leukemia cell lines. Combinations of CX-6258 with doxorubicin (10:1 molar ratio) and CX-6258 with paclitaxel (100:1 molar ratio) produces synergistic cell killing with combination index (CI50) values equal to 0.4 and 0.56, respectively. CX-6258 causes dose dependent inhibition of the phosphorylation of two pro-survival proteins, Bad and 4E-BP1, at the Pim kinase specific sites S112 and S65 and T37/46, respectively. [1]

激酶实验

Pim activity assay: 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.

Cas No.

1202916-90-2

分子式

C26H24ClN3O3

分子量

461.95

别名

CX 6258

储存和溶解度

DMSO:>10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years