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UNC2025
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。
UNC2025图片
CAS NO:1429881-91-3
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
1 mL*10 mM(in DMSO)电议

产品名称
mrx-6313
UNC 2025
UNC-2025
产品介绍
UNC2025 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。

产品描述

UNC-2025( IC50 of 0.74 nM and 0.8 nM) is a potent and orally bioavailable dual MER/FLT3 inhibitor. UNC-2025 is about 20-fold selectivity higher than Axl and Tyro3.

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]

Cas No.

1429881-91-3

分子式

C28H40N6O

分子量

476.7

别名

mrx-6313;UNC 2025;UNC-2025

储存和溶解度

Ethanol:8 mg/mL(15.59 mM),warming
H2O:100 mg/mL (194.88 mM)
DMSO:25 mg/mL(48.72 mM),warming
Powder: -20°C for 3 years
In solvent: -80°C for 2 years