CCT196969

Catalog No.S7743 Batch:S774301

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Technical Data

Formula

C27H24FN7O3
Molecular Weight 513.52 CAS No. 1163719-56-9
Solubility (25°C)* In vitro DMSO 100 mg/mL (194.73 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 Assay:[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 Study:[1]
  • Animal Models

    CD-1 mice

  • Dosages

    20 mg/kg 

  • Administration

    oral gavage

Selleck's CCT196969 has been cited by 2 publications

BRAF activation by metabolic stress promotes glycolysis sensitizing NRASQ61-mutated melanomas to targeted therapy [ Nat Commun, 2022, 13(1):7113] PubMed: 36402789
Genetic Heterogeneity of BRAF Fusion Kinases in Melanoma Affects Drug Responses. [ Cell Rep, 2019, 29(3):573-588] PubMed: 31618628

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.