CCT196969 (C09-0823-188)

InformationCCT196969 is a novel orally available, pan-RAFinhibitor with anti-SRCactivity. It also inhibits SRC, LCK, and the p38 MAPKs.TargetsCRAF (Cell-free assay); LCK (Cell-free assay); Src (Cell-free assay); V600E-BRAF (Cell-free assay); BRAF (Cell-free assay) ;0.01 μM; 0.02 μM; 0.03 μM; 0.04 μM; 0.1 μMIn vitroCCT196969 is active against melanoma and colorectal cancer cell lines that are mutant for BRAF, but not cancer cells that are wild-type for BRAF and NRAS. CCT196969 induces caspase 3 and PARP cleavage, thus induces apoptosis. CCT196969 does not drive paradoxical pathway activation and inhibit MEK/ERK in BRAF and NRAS mutant melanoma.In vivoCCT196969 is extremely well tolerated at the doses assessed and does not produce any significant adverse effects in vivo. Oral dosing at 10 mg/kg/day of CCT196969 results in plasma concentrations ∼1 μM at 24 hr. It is orally bioavailable at ∼55%.Cell Research(from reference)Cell lines：cell line derived from a vemurafenib-resistant melanoma Concentrations：1 μM Incubation Time：4 h. Specifications and Purity: 98%. Molecular Formula: C27H24FN7O3. Molecular Weight: 513.52. PubChem CID: 42628843. Isomeric SMILES: CC(C)(C)C1=NN(C(=C1)NC(=O)NC2=C(C=C(C=C2)OC3=C4C(=NC=C3)NC(=O)C=N4)F)C5=CC=CC=C5.