Free shipping on all orders over $ 500

MRTX-1257

Cat. No. M14054
MRTX-1257 Structure
Size Price Availability
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
Biological Activity

MRTX-1257 is a selective, irreversible, covalent and orally active KRAS G12C inhibitor, with an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells.

Chemical Information
Molecular Weight 565.71
CAS Number 2206736-04-9
Solubility (25°C) DMSO 55 mg/mL
Storage -20°C, sealed
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] Naveena Madhyastha, et al. Biomed Chromatogr. Validated HPLC-MS/MS method for quantitation of AMG 510, a KRAS G12C inhibitor, in mouse plasma and its application to a pharmacokinetic study in mice

Related Ras Products
KRpep-2d

KRpep-2d is a potent K-Ras inhibitor and inhibits proliferation of K-Ras-driven cancer cells.

Rac1 Inhibitor W56

Rac1 Inhibitor W56 is a peptide containing residues 45-60 of Rac1.

SAH-SOS1A

SAH-SOS1A is a peptide-based SOS1/KRAS protein interaction inhibitor.

Glecirasib

Glecirasib is a potent, irreversible, orally active KRAS G12C inhibitor for studies related to KRAS G12C-mediated cancers.

K20

K20 is a potent and selective KRas G12C inhibitor with an IC50 of 1.16 µM.

  Catalog
Abmole Inhibitor Catalog




Keywords: MRTX-1257 supplier, Ras, inhibitors, activators


Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.