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MRTX1133

MRTX1133
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Purity:99.10%
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MRTX1133

Catalog No. T9303Cas No. 2621928-55-8
MRTX1133 is a KRAS G12D inhibitor (KD=0.2 pM) that is potent, selective, and non-covalent. MRTX1133 exhibits inhibitory activity against KRAS G12D-mutated tumors, but not against KRAS wild-type tumors.
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Pack SizePriceAvailabilityQuantity
1 mg$197In Stock
5 mg$424In Stock
10 mg$649In Stock
25 mg$997In Stock
50 mg$1,420In Stock
100 mg$1,920In Stock
1 mL x 10 mM (in DMSO)$557In Stock
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Product Introduction

Bioactivity
Description
MRTX1133 is a KRAS G12D inhibitor (KD=0.2 pM) that is potent, selective, and non-covalent. MRTX1133 exhibits inhibitory activity against KRAS G12D-mutated tumors, but not against KRAS wild-type tumors.
In vitro
METHODS: Human gastric cancer cells AGS (KRASG12D) and MKN1 (KRASWT) were treated with MRTX1133 (0-3 μM) for 72 h, and cell viability was measured by CTG method in 2D culture.
RESULTS: The IC50 of MRTX1133 on AGS and MKN1 cells was 6 nM and >3000 nM, respectively. [1]
METHODS: Human gastric cancer cells AGS (KRASG12D) were treated with MRTX1133 (0-10 μM) for 3-72 h, and the expression levels of target proteins were detected by In-Cell Western method.
RESULTS: MRTX1133 inhibited the p-ERK level of AGS with an IC50 of 2 nM. [1]
METHODS: Human pancreatic cancer cells SUIT2 (KRASG12D) were treated with MRTX1133 (60 nmol/L) for 24 h, and the expression levels of target proteins were detected by Western Blot.
RESULTS: SUIT2 cells treated with MRTX1133 showed a significant decrease in pMEK1/2, a partial decrease in pERK1/2, and an initial decrease in pAKT followed by a recovery at a later time point. The levels of pEGFR and pHER2 decreased and recovered at 72 h. [2]
In vivo
METHODS: To test the antitumor activity in vivo, MRTX1133 (3-30 mg/kg, 10% Captisol in 50 mM citrate buffer pH 5.0) was intraperitoneally injected into nude-Foxn1nu mice bearing human pancreatic adenocarcinoma tumor Panc 04.03 twice daily for seven weeks.
RESULTS: MRTX1133 exhibited dose-dependent antitumor activity, with 94% tumor growth inhibition observed at the 3 mg/kg group. Tumor regression of -62% and -73% was observed in the 10 mg/kg and 30 mg/kg groups, respectively. [1]
METHODS: To assay antitumor activity in vivo, MRTX1133 (0.5 mg/kg in 12.5% Cremophor+12.5% ethanol+75%, orally once daily) and Cetuximab (50 mg/kg, intraperitoneally once weekly) were administered to BALB/c nude mice harboring human colorectal tumors, LS531 or CACO-2 for twenty-one days.
RESULTS: MRTX1133 significantly inhibited tumorigenesis in both in vivo models. The anti-tumor effect was further enhanced when MRTX1133 was combined with Cetuximab. [3]
Chemical Properties
Molecular Weight600.63
FormulaC33H31F3N6O2
Cas No.2621928-55-8
Storage & Solubility Information
Storage|Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
DMSO: 50 mg/mL (83.25 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.6649 mL8.3246 mL16.6492 mL83.2459 mL
5 mM0.3330 mL1.6649 mL3.3298 mL16.6492 mL
10 mM0.1665 mL0.8325 mL1.6649 mL8.3246 mL
20 mM0.0832 mL0.4162 mL0.8325 mL4.1623 mL
50 mM0.0333 mL0.1665 mL0.3330 mL1.6649 mL

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