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Chemical Structure : HH0043
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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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.
| M.Wt | 443.47 | |
| Formula | C23H24F3N5O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Li D, et al. ACS Med Chem Lett. 2024 Jun 3;15(6):958-964.
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