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Chemical Structure : IHMT-RAF-128
Catalog No.: 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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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.
| M.Wt | 507.52 | |
| Formula | C27H24F3N5O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Aoli Wang, et al. Eur J Pharmacol. 2023 May 8;175752.
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