MRTX1133

Catalog No.E1051 Batch:E105109

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Technical Data

Formula

C33H31F3N6O2
Molecular Weight 600.63 CAS No. 2621928-55-8
Solubility (25°C)* In vitro DMSO 100 mg/mL (166.49 mM)
 
 
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
5.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
5% DMSO 95% corn oil
1.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 20 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

MRTX1133 is a highly selective inhibitor of mutant KRAS G12D and can reversibly binds to the activated and inactivated KRAS G12D mutants and inhibit their activity. The specificity of MRTX1133 to KRAS G12D is more than 1000 times that of wild-type KRAS.
Targets
KRAS G12D [1]
In vitro

MRTX1133 not only possesses single-digit nM potency in a cellular proliferation assay, but also demonstrates tumor regressions in the Panc 04.03 xenograft model.
In vivo

MRTX1133 is a highly selective inhibitor of mutant KRAS G12D and can reversibly binds to the activated and inactivated KRAS G12D mutants and inhibit their activity. The specificity of MRTX1133 to KRAS G12D is more than 1000 times that of wild-type KRAS [2]

Protocol (from reference)

Animal Study:

[3]
  • Animal Models

    CD-1 mice

  • Dosages

    30 mg/kg

  • Administration

    i.p.

Selleck's MRTX1133 has been cited by 8 publications

Defining the KRAS- and ERK-dependent transcriptome in KRAS-mutant cancers [ Science, 2024, 384(6700):eadk0775] PubMed: 38843331
Determining the ERK-regulated phosphoproteome driving KRAS-mutant cancer [ Science, 2024, 384(6700):eadk0850] PubMed: 38843329
Macroautophagy/autophagy promotes resistance to KRASG12D-targeted therapy through glutathione synthesis [ Cancer Lett, 2024, 604:217258] PubMed: 39276914
Dual Inhibition of KRASG12D and Pan-ERBB Is Synergistic in Pancreatic Ductal Adenocarcinoma [ Cancer Res, 2023, 83(18):3001-3012] PubMed: 37378556
Feedback activation of EGFR/wild-type RAS signaling axis limits KRASG12D inhibitor efficacy in KRASG12D-mutated colorectal cancer [ Oncogene, 2023, 42(20):1620-1633] PubMed: 37020035
Feedback activation of EGFR/wild-type RAS signaling axis limits KRASG12D inhibitor efficacy in KRASG12D-mutated colorectal cancer [ Oncogene, 2023, 10.1038/s41388-023-02676-9 10.3322/caac.21660 10.1001/jama.2021.6021 10.1038/nrdp.2015.65 10.1038/s41575-019-0189-8 10.1038/nature11252 10.1038/s41392] PubMed: 37020035
Cetuximab Enhances the Efficacy of MRTX1133, a Novel KRASG12D Inhibitor, in Colorectal Cancer Treatment [ Anticancer Res, 2023, 43(10):4341-4348] PubMed: 37772552
Cetuximab Enhances the Efficacy of MRTX1133, a Novel KRASG12D Inhibitor, in Colorectal Cancer Treatment [ Anticancer Res, 2023, 43(10):4341-4348] PubMed: 37772552

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.