MRTX1133 |
رقم الكتالوجGC62699 |
MRTX1133 هو مثبط KRASG12D فعّال للغاية وانتقائي بتركيز عالي (<2nM).
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Cas No.: 2621928-55-8
Sample solution is provided at 25 µL, 10mM.
MRTX1133 is an exceptionally potent and selective KRASG12D inhibitor with high affinity (<2nM).[1]
In vitro, in the AGS cell line, MRTX1133 inhibited ERK phosphorylation with an IC50 of 2 nM. In the meanwhile, MRTX1133 was against the same cell line with an IC50 of 6 nM in a 2D viability assay.[1] In vitro efficacy test, in KRASG12D–mutant HPAC Cells, it indicated that treatment with 0.05 nM - 300 nM MRTX1133 has a dose-dependent pERK, pS6 & DUSP6 modulation.[2]
In vivo experiment it shown that treatment with 30 mg/kg of MRTX1133 intraperitoneally in CD-1 mice caused the sustained plasma exposure exceeding the free-fraction-adjusted pERK IC50 value in the KRASG12D mutant Panc 04.03 cell line for approximately 8 h. And in the Panc 04.03 xenograft tumor model, it suggested that MRTX1133 (3-30 mg/kg, i.p.) has 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.[1]
References:
[1].Wang X, Allen S, et al. Identification of MRTX1133, a Noncovalent, Potent, and Selective KRASG12D Inhibitor. J Med Chem. 2022 Feb 24;65(4):3123-3133.
[2].Swiatnicki M, Engel L, Shrestha R, Alves J, Goueli SA, Zegzouti H. Profiling oncogenic KRAS mutant drugs with a cell-based Lumit p-ERK immunoassay. SLAS Discov. 2022 Jun;27(4):249-257.
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