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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-Ras-pan-Ras inhibitor 3144
pan-Ras inhibitor 3144

Chemical Structure : pan-Ras inhibitor 3144

CAS No.: 1835283-94-7

pan-Ras inhibitor 3144 (Compound 3144)

货号: PC-62695Not For Human Use, Lab Use Only.

pan-Ras inhibitor 3144 (Compound 3144) is a multivalent small-molecule, pan-RAS inhibitor with Kd of 4.7/17/6.6/3.7 uM for KRAS G12D/KRAS wt/HRAS/NRAS respectively.

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纯度 & COA & 质检文件 纯度: 99.5% (LCMS) Select Batch:

生物&药学活性

pan-Ras inhibitor 3144 (Compound 3144) is a multivalent small-molecule, pan-RAS inhibitor with Kd of 4.7/17/6.6/3.7 uM for KRAS G12D/KRAS wt/HRAS/NRAS respectively.
pan-Ras inhibitor 3144 shows weak bindinf for RRAS2 (Kd=24 uM) and no activity for other small GTPases in the RAS superfamily.
pan-Ras inhibitor 3144 exhibits lethality in cells partially dependent on expression of RAS proteins.
pan-Ras inhibitor 3144 has suitable ADME properties and displays anti-tumor activity in xenograft mouse of pancreatic cancer; orally bioavailable.

物理化学性质&存储条件

分子量 717.659
分子式 C36H41Cl2F3N6O2
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

4-amino-N-(3-(5-((4-(2,6-dichlorobenzyl)piperazin-1-yl)methyl)-3-(4-(trifluoromethoxy)phenyl)-1H-indol-1-yl)propyl)piperidine-4-carboxamide

参考文献

1. Welsch ME, et al. Cell. 2017 Feb 23;168(5):878-889.e29.

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