MRTX1133 displays efficacious in a KRASG12D mutant xenograft mouse tumor model[1]. Animal Model: 6-8-weekold, female, athymic nude-Foxn1nu mice (Panc 04.03 model)[1] Dosage: 3, 10, or 30mg/kg Administration: Intraperitoneal; twice a day for 28 days Result: An antitumor efficacy study in this model resulted in MRTX1133 dose-dependent antitumor activity with 94% growth inhibition observed at 3 mg/kg BID (IP) and tumor regressions of −62% and −73% observed at 10 and 30 mg/kg BID (IP), respectively.
In Vitro
MRTX1133 inhibits ERK phosphorylation in the AGS cell line with an IC50 ranging 1-10 nM (AsPC-1, Panc 04.03, Panc 02.03, SW1990, GP2D, Suit2, A427, SNU1033, and HPAC cells). In a 2D viability assay, the IC50 of MRTX1133 is 6 nM against AGS cells (KRAS G12D), while demonstrating more than 500-fold selectivity against MKN1, a cell line which is dependent on KRAS for its growth and survival due to the amplification of wild-type KRAS[1].
Kinase Assay
Cell Assay
Animal Administration
References
[1]. Wang X, et al. Identification of MRTX1133, a Noncovalent, Potent, and Selective KRASG12D Inhibitor [published online ahead of print, 2021 Dec 10]. J Med Chem. 2021;10.1021/acs.jmedchem.1c01688.
[2]. KRAS G12D Inhibitor: MRTX1133. [(accessed on 22 April 2021)];2021 Available online
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