MRTX-1257

Catalog No.S8831 Batch:S883101

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Technical Data

Formula

C33H39N7O2
Molecular Weight 565.71 CAS No. 2206736-04-9
Solubility (25°C)* In vitro DMSO 100 mg/mL (176.76 mM)
Ethanol 30 mg/mL (53.03 mM)
Water Insoluble
* <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 MRTX-1257 is a potent, selective, irreversible, covalent and orally active inhibitor of KRAS G12C with IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells.
Targets
KRAS G12C [1] KRAS dependent ERK phosphorylation [1]
(in H358 cells)
900 pM
In vitro

MRTX1257 demonstrates rapid, irreversible modification of GDP-bound recombinant KRAS G12C and suppresses ERK phosphorylation with an IC50 = 1 nM in the H358 cell line. In proteomics studies designed to assess global protein modification, MRTX1257 is shown to be highly selective for the targeted Cys12 of KRAS G12C versus other surface-exposed cysteine residues in NCI-H358 cells.[2]
In vivo

MRTX1257 exhibits 31% bioavailability in mouse, demonstrates near-complete inhibition of KRAS signaling in tumor tissue, and complete durable tumor regression in MIA PaCa-2 xenografts.[2]

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    H358 Cells

  • Concentrations

    1 μM

  • Incubation Time

    --

  • Method

    --
Animal Study:

[1]
  • Animal Models

    mice

  • Dosages

    3 mg/kg, 30 mg/kg

  • Administration

    IV, Oral gavage

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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.