化合物ON123300 T6920

Product Introduction
Bioactivity


英文名: ON123300

描述: ON123300 是一种可透过血脑屏障的多激酶抑制剂，作用于 CDK4、CDK6、Ark5、PDGFRβ、FGFR1、RET 和 Fyn，IC50值为3.9、9.82、5、26、26、9.2和11 nM。它在脑肿瘤中抑制 Akt 磷酸化及激活 Erk。

激酶实验: CDK1 kinase activity is tested by the CDK1/cyclin B complex purified from baculovirus to phosphorylate a biotinylated peptide substrate containing the consensus phosphorylation site for histone H1, which is phosphorylated in vivo by CDK1. Inhibition of CDK1 activity is measured by observing a decreased amount of 33P-γ-ATP incorporation into the immobilized substrate in streptavidin-coated 96-well scintillating microplates. CDK1 enzyme is diluted in 50 mM Tris-HCl (pH 8), 10 mM MgCl2, 0.1 mM Na3VO4, 1 mM DTT, 1% DMSO, 0.25 μM peptide, 0.1 μCi per well 33P-γ-ATP, and 5 μM ATP in the presence or absence of various concentrations of JNJ-7706621 and incubated at 30 °C for 1 hour. The reaction is terminated by washing with PBS containing 100 mM EDTA and plates are counted in a scintillation counter. IC50 is determined by Linear regression analysis of the percent inhibition by JNJ-7706621.

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

溶解度: Ethanol : < 1 mg/mL (insoluble or slightly soluble)
H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 28 mg/mL (65.2 mM)


关键字: Platelet-derived growth factor receptor | ON123300 | AMP-activated protein kinase | FGFR1 | kinase | brain | CDK | Ark5 | U87 | inhibit | PDGFR | multi | RET | tumor | Inhibitor | glioma | Cyclin dependent kinase | AMPK | CDK4 | FYN | RTK | penetration | PDGFRβ | ON-123300 | CDK6 | ON 123300

相关产品: PD168393 | Masitinib | Mubritinib | S49076 HCl | FGFR4-IN-8 | LY2874455 | PRN1371 | Tyrosine kinase-IN-1 | Nintedanib esylate | S49076

相关库: Drug Repurposing Compound Library | AMPK-Targeted Compound Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Antidepressant Compound Library | Kinase Inhibitor Library | Inhibitor Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Active Compound Library | Tyrosine Kinase Inhibitor 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