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首页-小分子抑制剂&激动剂-Tyrosine Kinase-TAM Receptor (Tyro3-Axl-Mer)-UNC2025
UNC2025

Chemical Structure : UNC2025

CAS No.: 1429881-91-3

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UNC2025 (UNC 2025, UNC-2025)

货号: PC-42993Not For Human Use, Lab Use Only.

UNC2025 is a potent, orally bioavailable Mer/FLT3 dual inhibitor with IC50 of 0.74/0.8 nM, 700-fold less active against Met compared to Mer.

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10 mg ￥1180 In stock
25 mg ￥1980 In stock
50 mg ￥3480 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

UNC2025 is a potent, orally bioavailable Mer/FLT3 dual inhibitor with IC50 of 0.74/0.8 nM, 700-fold less active against Met compared to Mer.
UNC2025 also potently inhibits Axl and Tyro3 (IC50=14 and 17 nM) in vitro.
UNC2025 inhibits Mer phosphorylation (IC50=2.7 nM) in 697 B-ALL cells, decreases phosphorylation of Flt3 (IC50=14 nM) in Flt3-ITD positive Molm-14 AML cells.
UNC2025 effectively inhibits phosphorylation of Axl (IC50=122 nM) and Tyro3 (IC50=301 nM), 40- to 100-fold selectivity for Mer over Axl and Tyro3.
UNC2025 inhibits Mer phosphorylation in bone marrow leukemia cells in vivo.

物理化学性质&存储条件

分子量 476.6568
分子式 C28H40N6O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

DMSO: 33.33 mg/mL; H2O: < 4.9 mg/mL
Chemical Name/SMILES

Cyclohexanol, 4-[2-(butylamino)-5-[4-[(4-methyl-1-piperazinyl)methyl]phenyl]-7H-pyrrolo[2,3-d]pyrimidin-7-yl]-, trans-

参考文献

1. Zhang W, et al. J Med Chem. 2014 Aug 28;57(16):7031-41.

2. Cummings CT, et al. Mol Cancer Ther. 2015 Sep;14(9):2014-22.

3. DeRyckere D, et al. Clin Cancer Res. 2017 Mar 15;23(6):1481-1492.

4. Branchford BR, et al. J Thromb Haemost. 2018 Feb;16(2):352-363.

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