Home Apoptosis Ras inhibitor - ERK inhibitor MRTX-1257 For research use only.

MRTX-1257

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.

MRTX-1257 Chemical Structure

MRTX-1257 Chemical Structure

CAS No. 2206736-04-9

Purity & Quality Control

Batch: S883101 DMSO]100 mg/mL]false]Ethanol]30 mg/mL]false]Water]Insoluble]false Purity: 99.63%
99.63

MRTX-1257 Related Products

Signaling Pathway

Ras Signaling Pathways

Ras Signaling Pathway

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
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]
Cell Research Cell lines H358 Cells
Concentrations 1 μM
Incubation Time --
Method

--
In Vivo
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]
Animal Research Animal Models mice
Dosages 3 mg/kg, 30 mg/kg
Administration IV, Oral gavage

Chemical Information & Solubility

Molecular Weight 565.71 Formula

C33H39N7O2
CAS No. 2206736-04-9 SDF --
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (176.76 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 30 mg/mL

Water : Insoluble


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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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