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MRTX1133

MRTX1133

Manufacturer	MedChem Express
Category	Inhibitors
Type	Inhibitors
Specific against	other
Amount	100mg
Item no.	HY-134813-100mg
CASRN	2621928-55-8
Available
Product Description	MRTX1133 is a noncovalent, potent, and selective KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD 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.
StorageTemperature	Powder -20°C 3 years, 4°C 2 years; In solvent -80°C 6 months, -20°C 1 month
Formula	C33H31F3N6O2
References	[1]. KRAS G12D Inhibitor: MRTX1133. [(accessed on 22 April 2021)]; 2021 Available online. \| [2].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.
MolecularWeight	600.63
Research Area	Cancer
Solubility	DMSO : 50 mg/mL (83.25 mM; Need ultrasonic)
Target	Ras
Isoform	KRas G12D
Pathway	GPCR/G Protein

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Amount: 100mg

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Delivery expected until 4/13/2023

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