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ARS-1620

Cat. No. M9045
ARS-1620 Structure
Size Price Availability Quantity
5mg USD 210  USD210 In stock
10mg USD 330  USD330 In stock
25mg USD 560  USD560 In stock
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Quality Control & Documentation
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.

Chemical Information
Molecular Weight 430.84
Formula C21H17ClF2N4O2
CAS Number 1698055-85-4
Solubility (25°C) DMSO: ≥ 30 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] Hansen R, et al. Nat Struct Mol Biol. The reactivity-driven biochemical mechanism of covalent KRASG12C inhibitors.

[2] Janes MR, et al. Cell. Targeting KRAS Mutant Cancers with a Covalent G12C-Specific Inhibitor.

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