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Cat. No. M9045
ARS-1620 Structure
Size Price Availability Quantity
5mg USD 261  USD290 In stock
10mg USD 360  USD400 In stock
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Quality Control
Biological Activity

ARS-1620 exhibits complete growth suppression of p.G12C cell lines (IC50=150 nM) with relatively benign effects on control cell lines. ARS-1620 significantly reduces expression of the gene set in p.G12C mutant cells in a time-dependent manner but not in the p.G12S mutant cells.

In MIAPaCa2 xenografts (p.G12C), ARS-1620 significantly inhibits tumor growth (p<0.001) in a dose-dependent manner with marked regression at a dose of 200 mg/kg, given once daily. Across all tumor models employed, ARS-1620 is well tolerated over the entire 3-week treatment period.

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 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.

Chemical Information
Molecular Weight 430.84
Formula C21H17ClF2N4O2
CAS Number 1698055-85-4
Purity 99.81%
Solubility DMSO: ≥ 30 mg/mL
Storage at -20°C

The reactivity-driven biochemical mechanism of covalent KRASG12C inhibitors.
Hansen R, et al. Nat Struct Mol Biol. 2018 May 14. PMID: 29760531.

Targeting KRAS Mutant Cancers with a Covalent G12C-Specific Inhibitor.
Janes MR, et al. Cell. 2018 Jan 25;172(3):578-589.e17. PMID: 29373830.

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Abmole Inhibitor Catalog 2017

Keywords: ARS-1620 supplier, Ras, inhibitors

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