IHMT-RAF-128

Chemical Structure : IHMT-RAF-128

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货号: PC-20793Not For Human Use, Lab Use Only.

IHMT-RAF-128 is a highly potent pan-RAF inhibitor with IC50 of 5.9 and 3.6 nM for BRAF-V600E and CRAF, respectively.

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生物&药学活性

IHMT-RAF-128 is a highly potent pan-RAF inhibitor with IC50 of 5.9 and 3.6 nM for BRAF-V600E and CRAF, respectively.
IHMT-RAF-128 exhibits similarly high efficacies in inhibiting both partners of the RAF dimer.
IHMT-RAF-128 shows potent anti-tumor efficacy against a variety of cancer cells harboring either RAF or RAS mutations, especially Adagrasib and Sotorasib (AMG510) resistant-KRAS-G12C secondary mutations, such as KRAS-G12C-Y96C and KRAS-G12C-H95Q.
IHMT-RAF-128 shows excellent pharmacokinetic profile (PK), and the bioavailability in mice and rats were 63.9%, and 144.1%, respectively.
IHMT-RAF-128 exhibits potent anti-tumor efficacy on xenograft mouse tumor models in a dose-dependent manner without any obvious toxicities.

物理化学性质&存储条件

分子量	507.52
分子式	C27H24F3N5O2
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-(4-methyl-3-(4-(5-morpholinopyridin-3-yl)-1H-pyrazol-1-yl)phenyl)-3-(trifluoromethyl)benzamide

参考文献

1. Aoli Wang, et al. Eur J Pharmacol. 2023 May 8;175752.

IHMT-RAF-128

生物&药学活性

物理化学性质&存储条件

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IHMT-RAF-128

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物理化学性质&存储条件

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