HH0043 | SOS1 inhibitor | Probechem Biochemicals

Chemical Structure : HH0043

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HH0043 (HH-0043)

货号: PC-22561Not For Human Use, Lab Use Only.

HH0043 is a potent, orally bioavailable inhibitor of guanine nucleotide exchange factor (GEF) SOS1 with IC50 of 5.8 nM for KRAS/SOS1 binding inhibition, 54 nM for p-ERK inhibition.

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25 mg		Get quote
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100 mg		Get quote

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生物&药学活性

HH0043 is a potent, orally bioavailable inhibitor of guanine nucleotide exchange factor (GEF) SOS1 with IC50 of 5.8 nM for KRAS/SOS1 binding inhibition, 54 nM for p-ERK inhibition.
HH0043 displays 3-4 times more potent than BI-3406 with IC50 of 90 nM against NCI-H358 (human nonsmall lung cancer cell line) cells harboring KRASG12C mutation using 3D proliferative assay.
HH0043 exhibits n vivo antitumor activity in NCI-H358 human nonsmall lung cancer xenograft model harboring KRASG12C mutation, with a durable p-ERK inhibition.

物理化学性质&存储条件

分子量	443.47
分子式	C23H24F3N5O
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	(R)-1-(4-(4-((1-(3-(difluoromethyl)-2-fluorophenyl)ethyl)amino)-1,7-naphthyridin-6-yl)piperazin-1-yl)ethan-1-one

参考文献

1. Li D, et al. ACS Med Chem Lett. 2024 Jun 3;15(6):958-964.

HH0043 (HH-0043)

生物&药学活性

物理化学性质&存储条件

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HH0043 (HH-0043)

生物&药学活性

物理化学性质&存储条件

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