CCT196969

Catalog No.S7743

For research use only.

CCT196969 is a novel orally available, pan-RAF inhibitor with anti-SRC activity. It also inhibits SRC, LCK, and the p38 MAPKs.

CCT196969 Chemical Structure

CAS No. 1163719-56-9

Selleck's CCT196969 has been cited by 1 Publication

Purity & Quality Control

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Biological Activity

Description CCT196969 is a novel orally available, pan-RAF inhibitor with anti-SRC activity. It also inhibits SRC, LCK, and the p38 MAPKs.
Targets
CRAF [1]
(Cell-free assay)
LCK [1]
(Cell-free assay)
Src [1]
(Cell-free assay)
V600E-BRAF [1]
(Cell-free assay)
BRAF [1]
(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[1].

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%[1].

Protocol (from reference)

Cell Research:[1]
  • Cell lines: cell line derived from a vemurafenib-resistant melanoma
  • Concentrations: 1 μM
  • Incubation Time: 4 h
  • 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:[1]
  • Animal Models: CD-1 mice
  • Dosages: 20 mg/kg 
  • Administration: oral gavage

Solubility (25°C)

In vitro

DMSO 100 mg/mL
(194.73 mM)
Water Insoluble
Ethanol Insoluble

Chemical Information

Molecular Weight 513.52
Formula

C27H24FN7O3

CAS No. 1163719-56-9
Storage 3 years -20°C powder
2 years -80°C in solvent
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

In vivo Formulation Calculator (Clear solution)

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Molarity Calculator

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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