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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-Ras-Deltaflexin3
Deltaflexin3

Chemical Structure : Deltaflexin3

CAS No.: 2767277-64-3

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Deltaflexin3 (Deltaflexin 3)

货号: PC-22365Not For Human Use, Lab Use Only.

Deltaflexin3 is a highly potent, selective and highly soluble inhibitor of the trafficking chaperone PDE6D (PDEδ) with KD value of 6 nM, inhibits PDE6D/K-Ras binding and KRAS mutant cancer cell growth.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

Deltaflexin3 is a highly potent, selective and highly soluble inhibitor of the trafficking chaperone PDE6D (PDEδ) with KD value of 6 nM, inhibits PDE6D/K-Ras binding and KRAS mutant cancer cell growth.
Deltaflexin3 displays good selectivity for PDE6D-dependent and KRAS mutant with EC50 of 6 uM for MIA PaCa-2 (KRAS-G12C mutant) cells, as compared to HRAS mutant cancer cell lines.
Deltaflexin3 with the approved drug Sildenafil synergistically inhibit intracellular binding of K-Ras to PDE6D, more potently inhibits Ras signaling and microtumor growth.

物理化学性质&存储条件

分子量 457.59
分子式 C25H36FN5O2
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

N-(7-(ethyl((2-(methylamino)pyrimidin-4-yl)methyl)amino)-7-oxoheptyl)-4-fluoro-N-isopropylbenzamide

参考文献

1. Pelin Kaya, et al. J Med Chem. 2024 May 17. doi: 10.1021/acs.jmedchem.3c02129.

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