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ARS-853

Cat. No. M9235
ARS-853 Structure
Size Price Availability Quantity
2mg USD 324  USD360 In stock
5mg USD 585  USD650 In stock
10mg USD 994.5  USD1105 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

ARS-853 is a selective, covalent inhibitor of KRAS(G12C) that inhibits mutant KRAS-driven signaling by binding to the GDP-bound oncoprotein and preventing activation. ARS-853 reduces the level of GTP-bound KRAS by more than 95% (10 μM). ARS-853 inhibits proliferation with an inhibitory concentration 50% (IC50) of 2.5 μM, which is similar to its IC50 for target inhibition. ARS-853 (10 μM) inhibits effector signaling and cell proliferation to varying degrees in six KRASG12C mutant lung cancer cell lines. ARS-853 inhibits mutant KRAS-driven signaling by binding to the GDP-bound oncoprotein and preventing activation.

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 432.94
Formula C22H29ClN4O3
CAS Number 1629268-00-3
Purity >98%
Solubility DMSO: ≥ 45 mg/mL
Storage at -20°C
References

Allele-specific inhibitors inactivate mutant KRAS G12C by a trapping mechanism.
Lito P, et al. Science. 2016 Feb 5;351(6273):604-8. PMID: 26841430.

Selective Inhibition of Oncogenic KRAS Output with Small Molecules Targeting the Inactive State.
Patricelli MP, et al. Cancer Discov. 2016 Mar;6(3):316-29. PMID: 26739882.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: ARS-853 supplier, Ras, inhibitors

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