Identification of MRTX1133, a Noncovalent, Potent, and Selective ...
2021年12月10日 · KD and IC50 values were 51 and 8.9 nM, resp. After subsequent sequence optimization, we successfully generated KRpep-2d (Ac-RRRRCPLYISYDPVCRRRR-NH2) …
MRTX1133 is a potent, non-covalent KRASG12D inhibitor in vitro a,...
IC50 sensitivities ranged from 7 to 12 microM for 5-FU, 0.2-0.8 microM for ONC212, and >100 nM to >5,000 nM for MRTX1133 (G12D N=4: LS513 >100, HPAF-II >1,000, SNUC2B >5,000, …
Anti-tumor efficacy of a potent and selective non-covalent KRAS
2022年10月10日 · MRTX1133 inhibited ERK1/2 phosphorylation and cell viability in KRASG12D-mutant cell lines, with median IC50 values of ~5 nM, and demonstrated >1,000-fold selectivity …
KRASG12D inhibition reprograms the microenvironment of early …
Treatment of a human PDAC KRAS G12D mutant cell line (HPAC) and a murine PDAC Kras G12D mutant cell line (KPC689) with MRTX1133 resulted in effective downregulation of pERK …
MRTX1133 | KRAS G12D抑制剂 | MCE - MCE-生物活性分子大师
MRTX1133 抑制 AGS 细胞系中的 ERK 磷酸化，IC 50 范围为 1-10 nM（AsPC-1、Panc 04.03、Panc 02.03、SW1990、GP2D、Suit2、A427、SNU1033 和 HPAC 细胞）。
MRTX1133抑制剂 - 知乎 - 知乎专栏
MRTX1133 抑制AGS细胞ERK 磷酸化 的IC50值为1-10 nM （AsPC-1、Panc 04.03、Panc 02.03、SW1990、GP2D、Suit2、A427、SNU1033和HPAC细胞）。 在2D活力试验 …
growth arrest and/or regression in multiple PDAC (HPAC, Panc 04.03, and 2838c3) and CRC (CT26, GP2D, and LS513) mouse tumor models. These preclinical results demonstrate that …
Discovery of Prodrug of MRTX1133 as an Oral Therapy for Cancers …
2023年2月9日 · In this study, we evaluated the mechanism of action and anti-tumor efficacy of MRTX1133, a potent, selective and non-covalent KRASG12D inhibitor. MRTX1133 …
【MRTX1133】MRTX1133 CAS号:2621928-55-8【结构式 性质 活 …
MRTX1133在IC50范围为1-10nm的AGS细胞系中抑制ERK磷酸化(AsPC-1、Panc 04.03、Panc 02.03、SW1990、GP2D、Suit2、A427、SNU1033和HPAC细胞)。 在2D活性测定 …
Results: The PARP1 IC50 values for CFPAC-1, BXPC-3 and. (52.6 μM, 100.9 μM 102.0 μM) and Olaparib (79.5 μM, 184.8 μM, 200.2 μM). The IC50 values. clinically relevant amounts of …