化合物CX-6258 HCl T6148

Product Introduction
Bioactivity


英文名: CX-6258 hydrochloride

描述: 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。

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.

体外活性: CX-6258 has anti-proliferative activity against a panel of human cancer cell lines (IC50: 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 (CI50: 0.4 and 0.56).

体内活性: In mice carrying MV-4-11 xenografts, CX-6258 dose-dependently suppresses the tumor growth , with a 50/100 mg/kg dose producing 45%/75% tumor growth inhibition.

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

溶解度: H2O : 82 mg/mL (164.5 mM)
DMSO : 53 mg/mL (106.3 mM)
Ethanol : 1 mg/mL (2.0 mM)


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

相关产品: Pim-1 kinase inhibitor 8 | Neoprzewaquinone A | (2R)-Octyl-α-hydroxyglutarate | Hispidulin | XL413 hydrochloride | K00135 | Uzansertib phosphate | PIM1-IN-4 | TP-3654 | BMS-863233 HCl

相关库: JAK-STAT Compound Library | Anti-Cancer Compound Library | Anti-Lung Cancer Compound Library | Bioactive Compounds Library Max | Kinase Inhibitor Library | Inhibitor Library | Epigenetics Compound Library | Anti-Cancer Active Compound Library | Covalent Inhibitor Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途