化合物UNC2025 T7007

Product Introduction
Bioactivity


英文名: UNC2025

描述: UNC2025 (mrx-6313) 是高效的、具有口服活性的、ATP 竞争性的Mer/Flt3双抑制剂，IC50值分别为 0.74 nM 和 0.8 nM。它对MERTK 的选择性比 Axl 高 45 倍(IC50:122 nM;Ki:13.3 nM)。它具有良好的 PK 特性，可用于研究急性白血病。

体外活性: In 697 B-ALL cells, UNC-2025 potently inhibits Mer phosphorylation with IC50 of 2.7 nM. In A549 NSCLC and Molm-14 AML cell lines, UNC-2025 causes significant inhibition of colony formation dependent on Mer8 and Flt3. [1] In H2228 and H1299 cell lines, UNC-2025 inhibits MERTK oncogenic signaling downstream, such as basal and stimulated pAKT and pERK1/2. In four NSCLC cell lines, UNC-2025 also induces apoptotic cell death, and decreases colony formation. [2]

体内活性: In mice bearing 697 acute leukemia tumors, UNC-2025 (3 mg/kg, p.o.) shows good solubility and DMPK properties, and results in effective target inhibition. [1] In mice bearing H2228 or A549 tumors, UNC-2025 (50 mg/kg, p.o.) inhibits tumor growth. [2]

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

溶解度: H2O : Insoluble
Ethanol : 8 mg/mL(15.59 mM)
DMSO : 6.25 mg/mL (13.11 mM)


关键字: UNC2025 | Inhibitor | inhibit | FLT3 | leukemia | CD135 | Fms like tyrosine kinase 3 | acute | Cluster of differentiation antigen 135 | cancer | MERTK

相关产品: Edicotinib | Crenolanib | SGI-1776 | Sunitinib | OSI-930 | UNC2025 2HCl (1429881-91-3(free base)) | R406 free base | Sorafenib | GSK-1070916 | FLT3-IN-4

相关库: Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Kinase Inhibitor Library | Inhibitor Library | Tyrosine Kinase Inhibitor Library | Anti-Cancer Active Compound Library | Hematonosis Compound Library | Orally Active Compound Library | NO PAINS Compound 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