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CCT196969 - 10mM in DMSO, high purity , CAS No.1163719-56-9
C-Raf/Raf-1 Selective Inhibitors
Basic Description Specifications & Purity Moligand™, 10mM in DMSO Biochemical and Physiological Mechanisms CCT196969 is a novel orally available, pan-RAF inhibitor with anti-SRC activity. It also inhibits SRC, LCK, and the p38 MAPKs. Storage Temp Store at -80°C Shipped In Ice chest + Ice pads Grade Moligand™ Product Description Information
CCT196969 is a novel orally available, pan-RAFinhibitor with anti-SRCactivity. It also inhibits SRC, LCK, and the p38 MAPKs.
Targets
CRAF (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 μM
In vitro
CCT196969 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 vivo
CCT196969 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
Associated Targets(Human) Associated Targets(non-human) Mechanisms of Action Mechanism of Action Action Type target ID Target Name Target Type Target Organism Binding Site Name References
Names and Identifiers IUPAC Name 1-(5-tert-butyl-2-phenylpyrazol-3-yl)-3-[2-fluoro-4-[(3-oxo-4H-pyrido[2,3-b]pyrazin-8-yl)oxy]phenyl]urea INCHI InChI=1S/C27H24FN7O3/c1-27(2,3)21-14-22(35(34-21)16-7-5-4-6-8-16)32-26(37)31-19-10-9-17(13-18(19)28)38-20-11-12-29-25-24(20)30-15-23(36)33-25/h4-15H,1-3H3,(H,29,33,36)(H2,31,32,37) InChi Key KYYKGSDLXXKQCR-UHFFFAOYSA-N Canonical 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 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 PubChem CID 42628843 MeSH Entry Terms 1-(3-tert-butyl-1-phenyl-1H-pyrazol-5-yl)-3-(2-fluoro-4-(3-oxo-3,4-dihydropyrido(3,2-b)pyrazin-8-yloxy)phenyl)urea;CCT196969 Molecular Weight 513.52
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