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CEP-32496 is a novel RAF inhibitor with IC50 values of 14 nM, 36 nM, 39 nM, 3 nM and 9 nM for BRAF(V600E), BRAF(WT), c-Raf, Abl-1 and CSF-1R, respectively. CEP-32496 is orally bioavailable in multiple preclinical species (>95% in rats, dogs, and monkeys) and has single oral dose pharmacodynamic inhibition (10-55 mg/kg) of both pMEK and pERK in BRAF(V600E) colon carcinoma xenografts in nude mice. In vitro, CEP-32496 has multikinase binding activity at other cancer targets of interest; however, it exhibits selective cellular cytotoxicity for BRAF(V600E) versus wild-type cells. CEP-32496 exhibits high potency against several BRAF(V600E)-dependent cell lines and selective cytotoxicity for tumor cell lines expressing mutant BRAF(V600E) versus those containing wild-type BRAF. CEP-32496 also exhibits an excellent PK profile across multiple preclinical species. In addition, significant oral efficacy was observed in a 14-day BRAF(V600E)-dependent human Colo-205 tumor xenograft mouse model, upon dosing at 30 and 100 mg/kg BID.
| Molecular Weight | 517.46 |
| Formula | C24H22F3N5O5 |
| CAS Number | 1188910-76-0 |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Raf Products |
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Vemurafenib (PLX4032) is a first-in-class, potent, selective inhibitor of B-Raf that inhibits RAFV600E and C-RAF-1 activity with IC50s of 31 nM and 48 nM, respectively.In addition, Vemurafenib induces autophagy. |
| PLX-4720
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| SB590885
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| ZM 336372
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