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CCT196969

CCT196969
CCT196969 is a novel orally available, pan-RAF inhibitor with anti-SRC activity. It also inhibits SRC, LCK, and the p38 MAPKs.
Catalog No. T4133Cas No. 1163719-56-9
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Purity:99.65%
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CCT196969

Catalog No. T4133Cas No. 1163719-56-9

CCT196969 is a novel orally available, pan-RAF inhibitor with anti-SRC activity. It also inhibits SRC, LCK, and the p38 MAPKs.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
Pack SizePriceAvailabilityQuantity
2 mg$30In Stock
5 mg$48In Stock
10 mg$77In Stock
25 mg$163In Stock
50 mg$263In Stock
100 mg$428In Stock
1 mL x 10 mM (in DMSO)$54In Stock
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Product Introduction

Bioactivity
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
Src:0.03 μM, B-Raf (V600E):0.04 μM, Raf:0.01 μM, BRAF:0.1 μM, Lck:0.02 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
Chemical Properties
Molecular Weight513.52
FormulaC27H24FN7O3
Cas No.1163719-56-9
Storage & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM1.9473 mL9.7367 mL19.4734 mL97.3672 mL
5 mM0.3895 mL1.9473 mL3.8947 mL19.4734 mL
10 mM0.1947 mL0.9737 mL1.9473 mL9.7367 mL
20 mM0.0974 mL0.4868 mL0.9737 mL4.8684 mL
50 mM0.0389 mL0.1947 mL0.3895 mL1.9473 mL
100 mM0.0195 mL0.0974 mL0.1947 mL0.9737 mL

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