Extended Data Fig. 5: Pathology and anti-tumor activity of MRTX1133 in an orthotopic pancreatic cancer xenograft model.
From: Anti-tumor efficacy of a potent and selective non-covalent KRASG12D inhibitor
(a) Bioluminescent imaging of luciferase-labeled KRASG12D-mutant AsPC-1 tumors orthotopically implanted into the pancreas of immunocompromised mice. Starting on day 7 after implant, MRTX1133 was administered i.p. BID at 30 mg/kg to mice for 28 days (n = 6/group). (b) Abdominal photon flux from mice in A. Data are shown as mean abdominal bioluminescent imaging flux+/− SEM. ‘*’ indicated tumor bioluminescence at ~Day 28 for MRTX1133 treated mice were statistically significant vs vehicle using a two-tailed Student’s t-test (p-value <0.05). (c) Tumor H&E stains from vehicle and MRTX1133-treated tumors collected and processed at the end of the study. Scale for 10X images is 300um, 20X images is 200um. (d) ERK1/2 (Thr202/Tyr204) modulation at 1 and/or 6 hours post last dose was evaluated from tumors treated with Vehicle or MRTX1133 after BID + 1 dosing schedule (n = 3/time point) or BID × 28 days (n = 4 mice per time point) in AsPC-1 pancreatic orthotopic tumors. Data are shown as mean+/− standard deviation (SD).
