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首页-小分子抑制剂&激动剂-Tyrosine Kinase-TAM Receptor (Tyro3-Axl-Mer)-UNC3810A
UNC3810A

Chemical Structure : UNC3810A

CAS No.: 1818233-86-1

UNC3810A (UNC-3810A, UNC3810)

货号: PC-24219Not For Human Use, Lab Use Only.

UNC3810A (UNC3810) is a potent, selective Tyro3 kinase inhibitor of IC50 of 1.2 nM, >10-fold selectivity versus all other kinases beyond MerTK, the most closely related TAM member, and TRKA.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

UNC3810A (UNC3810) is a potent, selective Tyro3 kinase inhibitor of IC50 of 1.2 nM, >10-fold selectivity versus all other kinases beyond MerTK, the most closely related TAM member, and TRKA.
UNC3810A induces dose-dependent decrease of Tyro3 phosphorylation and attenuates signaling through the PI3K/AKT/mTOR pathway as evidenced by decreased phosphorylation of p85 PI3K and AKT in both HT-29 and B16-F10 cells.
UNC3810A (0.5-1 uM) resulted in a significant attenuation in the formation of colonies for the primary effusion lymphoma (PEL) lines, but not in other NHL subtypes where Tyro3 was not highly expressed.
UNC3810A (25 mg/kg, 3 times a week, i.p.) retards PEL tumor growth in NOD-SCID mice in a BCBL1-PEL xenograft model.

物理化学性质&存储条件

分子量 504.72
分子式 C30H44N6O
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

10 mM in DMSO

Chemical Name/SMILES

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

参考文献

1. Wong JP, et al. Proc Natl Acad Sci U S A. 2019 Aug 13;116(33):16541-16550.

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