化合物CX-6258 T1834

Product Introduction
Bioactivity


英文名: CX-6258

描述: CX-6258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。

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.

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]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 22.5 mg/mL (48.71 mM)


关键字: CX6258 | Pim kinases | Inhibitor | inhibit | Bad | Pim | 4E-BP1 | CX-6258

相关产品: BRD7389 | Pim-1/2 kinase inhibitor 1 | GDC-0339 | XL413 | SGI-1776 | Pim-1 kinase inhibitor 5 | M-110 | GNE-955 | BMS-863233 HCl | Pim-1 kinase inhibitor 4

相关库: Anti-Prostate Cancer Compound Library | Anti-Liver Cancer Compound Library | Anti-Cancer Compound Library | Anti-Lung Cancer Compound Library | Bioactive Compounds Library Max | Kinase Inhibitor Library | Inhibitor Library | Epigenetics Compound Library | Anti-Pancreatic Cancer Compound Library | Bioactive Compound Library

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