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Cat. No.: HY-134813R

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MRTX1133 (Standard)

MRTX1133 (Standard) is the analytical standard of MRTX1133 (HY-134813). This product is intended for research and analytical applications. MRTX1133 is a noncovalent, potent, and selective alkyne-based KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated K_D against KRAS G12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations.

For research use only. We do not sell to patients.

CAS No.: 2621928-55-8
Formula: C₃₃H₃₁F₃N₆O₂
Molecular Weight:600.63

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

MRTX1133 (Standard) Chemical Structure

CAS No.: 2621928-55-8

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

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Application

The compound is the grade of analytical standard, which is the reference standard supplied assay. It is commonly used in qualitative, quantitative and methodological research experiments in HPLC, GC and MS.

Chemical Information

CAS No. 2621928-55-8
Molecular Weight 600.63
Formula C₃₃H₃₁F₃N₆O₂
SMILES

OC1=CC(C2=C(F)C3=NC(OC[C@]45C[C@@H](F)CN4CCC5)=NC(N6C[C@H]7N[C@H](CC7)C6)=C3C=N2)=C8C(C#C)=C(F)C=CC8=C1
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Wang X, et al. Identification of MRTX1133, a Noncovalent, Potent, and Selective KRAS G12D Inhibitor [published online ahead of print, 2021 Dec 10]. J Med Chem. 2021;10.1021/acs.jmedchem.1c01688. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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