CCT196969

Catalog No.S7743

CCT196969 Chemical Structure

Molecular Weight(MW): 513.52

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

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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

Cell Research:[1]
+ Expand
  • 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).
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: CD-1 mice
  • Formulation: 5% DMSO, 95% water
  • Dosages: 20 mg/kg 
  • Administration: oral gavage
    (Only for Reference)

Solubility (25°C)

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

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 513.52
Formula

C27H24FN7O3

CAS No. 1163719-56-9
Storage powder
in solvent
Synonyms N/A

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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

Tel: +1-832-582-8158 Ext:3

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Raf Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID