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CCT239065

Cat. No. M3196

CCT239065 Structure
Size Price Availability Quantity
5mg USD 220 In stock
10mg USD 300 In stock
50mg USD 860 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

CCT239065 is a novel, selective, and efficacious nanomolar pyridopyrazinone V600EBRAF and LCK inhibitor with IC50 of 13 and 6 nM, respectively. CCT239065 is active against oncogenic BRAF in cells. CCT239065 also inhibits BRAF, CRAF and SRC with IC50 of 81, 12 and 23 nM, respectively. CCT239065 is more than 6-fold less active against wild-type BRAF and more than 50-fold less active against EGFR2/KDR than against V600EBRAF. CCT239065 inhibits ERK1/2 phosphorylation at 5 nM in WM266.4 cells. CCT239065 achieves high levels of selectivity in vitro and at 1 μM, a concentration that is approximately 50 times higher than its IC50 value against purified V600EBRAF. CCT239065 reveals a very low plasma clearance (0.4 mL/hour) consistent with the absence of metabolism and a terminal half-life of 6.8 hours.Plasma concentrations of CCT239065 achieve over 100-fold greater than the average GI50 value for BRAF mutant cancer cell lines in vitro and are sustained above the average GI50 in plasma and muscle (used as a tumor tissue surrogate) for over 18 hours. CCT239065 is well tolerated in mice and displays excellent oral bioavailability. Inhibition of V600EBRAF-mediated signaling in human tumor xenografts is observed following oral administration of a single dose of CCT239065.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 555.65
Formula C29H29N7O3S
CAS Number 1163719-51-4
Purity >99%
Solubility DMSO
Storage at -20°C
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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: CCT239065 supplier, DNA/RNA Synthesis, inhibitors

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