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CCT196969

Cat. No. M20609
CCT196969 Structure
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Biological Activity

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

Chemical Information
Molecular Weight 513.52
Formula C27H24FN7O3
CAS Number 1163719-56-9
Solubility (25°C) DMSO 100 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Agathe Reigstad, et al. PLoS One. CCT196969 effectively inhibits growth and survival of melanoma brain metastasis cells

[2] Gautham Gampa, et al. J Pharmacol Exp Ther. Brain Distribution and Active Efflux of Three panRAF Inhibitors: Considerations in the Treatment of Melanoma Brain Metastases

[3] Maria Romina Girotti, et al. Cancer Cell. Paradox-breaking RAF inhibitors that also target SRC are effective in drug-resistant BRAF mutant melanoma

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  Catalog
Abmole Inhibitor Catalog




Keywords: CCT196969 supplier, Raf, inhibitors, activators


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