Chemical Structure : HH0043
CAS No.:
2922069-42-7
HH0043
(HH-0043)
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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443.47
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Formula
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C23H24F3N5O
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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(R)-1-(4-(4-((1-(3-(difluoromethyl)-2-fluorophenyl)ethyl)amino)-1,7-naphthyridin-6-yl)piperazin-1-yl)ethan-1-one
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References
1. Li D, et al. ACS Med Chem Lett. 2024 Jun 3;15(6):958-964.
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