Free shipping on all orders over $ 500

ARS-1620

Cat. No. M9045
ARS-1620 Structure
Size Price Availability Quantity
5mg USD 261  USD290 In stock
10mg USD 360  USD400 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

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
References

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.

Related Ras Products
CID-1067700 (ML282)

CID-1067700 (ML282) is a competitive inhibitors of nucleotide binding by Ras-related GTPases with a Ki of 13 nM for Rab7.

MLS000532223

MLS000532223 is a selective inhibitor of Rho family GTPases, with EC50 ranging from 16 μM to 120 μM.

BI-3406

BI-3406 is a highly potent and selective SOS1::KRAS inhibitor (IC50=6 nM), which selectively binds to SOS1 and blocks the interaction with KRAS, irrespective of the KRAS mutation.

ZT-12-037-01

ZT-12-037-01 is a potent, selective, ATP-competitive STK19 inhibitor with IC50 values of 23.96 nM and 27.94 nM for STK19 (WT) and STK19 (D89N), respectively.

BI-2852

BI-2852 is a potent KRAS inhibitor that binds with nanomolar affinity to a pocket.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: ARS-1620 supplier, Ras, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.