MRTX-1257 Inhibitor

Name: MRTX-1257 Inhibitor; MyBioSource
Brand: MyBioSource
SKU: MBS5755229
Availability: InStock
Rating: 5 (10 reviews)

For Research Use Only. Not for use in diagnostic procedures. Catalog #: MBS5755229

MRTX-1257 is a selective, irreversible, and covalent inhibitor of KRAS G12C. It has an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells.MRTX1257 demonstrated 31% bioavailability in the mouse, with free fraction exposures well above the… More details

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Product Documentation

Sample Manual Insert View PDF

Testing Data View PDF

Certificate of Analysis (COA) View PDF

QC Report View PDF

Material Safety Data Sheet View PDF

Technical Datasheet View PDF

Protocol View PDF

Product Overview

Online Datasheet in PDF

Product Name

MRTX-1257, Inhibitor

Full Product Name

MRTX-1257

Product Gene Name

MRTX-1257, inhibitor

Form/Format

Solid. Powder

Purity/Purification

98.00%

Preparation and Storage

Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent

Molecular Weight

565.71

Solubility

DMSO: 54mg/mL (95.46mM)
(<1mg/ml refers to the product slightly soluble or insoluble)

Formula

C33H39N7O2

SMILES

CN1CCC[C@H]1COc1nc2CN(CCc2c(n1)N1CCN([C@@H](CC#N)C1)C(=O)C=C)c1cccc2cccc(C)c12

CAS Number

2206736-04-9

Target & IC50

KRAS(G12C)

In Vitro

MRTX-1257 shows sustained regression at 3,10, 30, and 100mg/kg dose groups. MRTX-1257 dosed of 100mg/kg daily causes complete responses that are maintained >70 days after cessation of treatment, MRTX-1257 (1mg/kg, 3mg/kg, 10mg/kg, 30mg/kg and 100mg/kg, orally, daily for 30 days) displays rapid tumor growth inhibition at all dose groups in MIA PaCa-2 G12C Xenograft model in mice.

Product Categories/Family for MRTX-1257, inhibitor

GPCR/G Protein; MAPK

Product References and Citations for MRTX-1257, inhibitor

Matthew et al. Structure-Based Drug Discovery of MRTX1257, a Selective, Covalent KRAS G12C Inhibitor with Oral Activity in Animal Models of Cancer.

Other Notes

Small volumes of MRTX-1257, inhibitor vial(s) may occasionally become entrapped in the seal of the product vial during shipment and storage. If necessary, briefly centrifuge the vial on a tabletop centrifuge to dislodge any liquid in the container`s cap. Certain products may require to ship with dry ice and additional dry ice fee may apply.

Searchable Terms for MRTX-1257 purchase

MBS5755229 is an inhibitor targeting MRTX-1257.