1. GPCR/G Protein
  2. Ras
  3. MRTX-1257

MRTX-1257 

Cat. No.: HY-114436
Handling Instructions

MRTX-1257 is a selective, irreversible, covalent and oral active KRAS G12C inhibitor, with an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells.

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

MRTX-1257 Chemical Structure

MRTX-1257 Chemical Structure

CAS No. : 2206736-04-9

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Description

MRTX-1257 is a selective, irreversible, covalent and oral active KRAS G12C inhibitor, with an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells[1].

IC50 & Target

IC50: 900 pM (KRAS dependent ERK phosphorylation in H358 cells)[1].

In Vivo

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

Animal Model: MIA PaCa-2 G12C Xenograft Model (mouse)[1].
Dosage: 1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg and 100 mg/kg.
Administration: Orally daily for 30 days.
Result: Showed rapid tumor growth inhibition at all dose groups.
Showed sustained regression at 3,10, 30, and 100 mg/kg dose groups.
100 mg/kg daily led to complete responses that are maintained >70 days after cessation of treatment.
Storage

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

References
Molecular Weight

565.71

Formula

C₃₃H₃₉N₇O₂

CAS No.

2206736-04-9

SMILES

N#CC[[email protected]@H]1N(C(C=C)=O)CCN(C2=C3C(CN(C4=C5C(C)=CC=CC5=CC=C4)CC3)=NC(OC[[email protected]]6N(C)CCC6)=N2)C1

Shipping

Room temperature in continental US; may vary elsewhere

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MRTX-1257
Cat. No.:
HY-114436
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MRTX-1257

Cat. No.: HY-114436