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CCT196969 is a novel orally available, pan-RAF inhibitor with anti-SRC activity. It also inhibits SRC, LCK, and the p38 MAPKs.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | $30 | In Stock | |
5 mg | $48 | In Stock | |
10 mg | $77 | In Stock | |
25 mg | $163 | In Stock | |
50 mg | $263 | In Stock | |
100 mg | $428 | In Stock | |
1 mL x 10 mM (in DMSO) | $54 | In Stock |
Description | CCT196969 is a novel orally available, pan-RAF inhibitor with anti-SRC activity. It also inhibits SRC, LCK, and the p38 MAPKs. |
Targets&IC50 | B-Raf (V600E):0.04 μM, Src:0.03 μM, Lck:0.02 μM, Raf:0.01 μM, BRAF:0.1 μM |
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. |
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 |
Molecular Weight | 513.52 |
Formula | C27H24FN7O3 |
Cas No. | 1163719-56-9 |
Smiles | CC(C)(C)c1cc(NC(=O)Nc2ccc(Oc3ccnc4[nH]c(=O)cnc34)cc2F)n(n1)-c1ccccc1 |
Relative Density. | no data available |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | Ethanol: Insoluble DMSO: 100 mg/mL (194.73 mM) H2O: Insoluble | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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