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首页-小分子抑制剂&激动剂-Tyrosine Kinase-TAM Receptor (Tyro3-Axl-Mer)-CPL423
CPL423

Chemical Structure : CPL423

CAS No.:

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CPL423 (CPL-423)

货号: PC-26514Not For Human Use, Lab Use Only.

CPL423 is a potent selective TAM family of receptor tyrosine kinases (TYRO3, AXL, MERTK) and FLT inhibitor with IC50 of MERTK (0.47 nM) and FLT3 (0.94 nM), inhibits AXL and TYRO3 with IC50 of 2.15 and 6.73 nM, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

CPL423 is a potent selective TAM family of receptor tyrosine kinases (TYRO3, AXL, MERTK) and FLT inhibitor with IC50 of MERTK (0.47 nM) and FLT3 (0.94 nM), inhibits AXL and TYRO3 with IC50 of 2.15 and 6.73 nM, respectively.
CPL423 demonstrates markedly reduced activity against other kinases, with IC50 values of 60.35 nM for PDGFRβ, 71.91 nM for TrkA, 221.90 nM for TrkC, and 13900 nM for TrkB.
CPL423 exhibits potent, dose-dependent cytotoxic activity. The IC50 was 5.7 nM in MOLM-13 cells and 7.92 nM in MV4-11 cells.
CPL423 reduces cell viability with an IC50 of 388.1 nM in A375 melanoma cell line.
CPL423 reduces MERTK phosphorylation (pMERTK) in a dose-dependent manner across 1–250 nM in MERTK-stable Ba/F3 cells, reduces phosphorylation of AKT and ERK.
CPL423 reduces the phagocytic capacity of bone marrow-derived mouse dendritic cells (BMDCs).
CPL423 (30 to 50 mg/kg, orally, once daily (QD)) demonstrates antitumor activity in MOLM-13 xenograft model.

物理化学性质&存储条件

分子量 474.65
分子式 C28H38N6O
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

(1r,4r)-4-(2-(but-3-en-1-ylamino)-5-(4-((4-methylpiperazin-1-yl)methyl)phenyl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)cyclohexan-1-ol

参考文献

1. Mikołajczyk A, et al. Front Pharmacol. 2026 Mar 25;17:1768167.

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