| Name | CCT196969 |
| Description | CCT196969 is a novel orally available, pan-RAF inhibitor with anti-SRC activity. It also inhibits SRC, LCK, and the p38 MAPKs. |
| Cell Research | Cell lines: cell line derived from a vemurafenib-resistant melanoma. Method: The three cell lines derived from tumors displaying resistance to vemurafenib are incubated with DMSO (control),PLX4720,CCT196969,or CCT241161 (1 μM; 4 hr).Protein extracts are prepared in CLB1 lysis buffer,and samples are analyzed by Zeptosens RPPA(reverse phase protein arrays). |
| Animal Research | Animal Models: CD-1 mice. Formulation: 5% DMSO,95% water. Dosages: 20 mg/kg . Administration: oral gavage |
| In vitro | 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. 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. |
| 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%. CCT196969 is extremely well tolerated at the doses assessed and does not produce any significant adverse effects in vivo. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 4 mg/mL (7.79 mM), Sonication is recommended.
Ethanol : Insoluble
DMSO : 127.5 mg/mL (248.29 mM), Sonication is recommended.
H2O : Insoluble
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| Keywords | Src | Raf kinases | Raf | Inhibitor | inhibit | C-RAF | CCT-196969 | CCT196969 | CCT 196969 |
| Inhibitors Related | Regorafenib monohydrate | Nintedanib | Exarafenib | Vemurafenib | Sorafenib | Dasatinib | Ibrutinib | Regorafenib | Dabrafenib | iHCK-37 | MCB-613 | RMC-7977 |
| Related Compound Libraries | Anti-Colorectal Cancer Compound Library | Pain-Related Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | Angiogenesis related Compound Library | Inhibitor Library | Anti-Prostate Cancer Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library |
United States
