Product Description
MRTX-1257 is a potent, selective, and irreversible covalent inhibitor of KRAS G12C. MRTX-1257 inhibits KRAS dependent ERK-phosphorylation in the H358 cell with IC₅₀ of 0.9 nM. Displays high selectivity for the Cys12 of KRAS G12C in NCI-H358 cells over other cysteines. Exhibits robust target engagement in vivo.
MRTX-1257 is a potent, selective, and irreversible covalent inhibitor of KRAS G12C. MRTX-1257 inhibits KRAS dependent ERK-phosphorylation in the H358 cell with IC₅₀ of 0.9 nM. Displays high selectivity for the Cys12 of KRAS G12C in NCI-H358 cells over other cysteines. Exhibits robust target engagement in vivo.
Biovision | B2614 | MRTX-1257 DataSheet
Alternate Name/Synonyms: MRTZ1257, 2-((S)-1-acryloyl-4-(7-(8-methylnaphthalen-1-yl)-2-(((S)-1-methylpyrrolidin-2-yl)methoxy)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-yl)piperazin-2-yl)acetonitrile, MRTX1257
Appearance: White to off-white solid
Formulation:
CAS Number: 2206736-04-9
Structure Available?: Yes
Peptide sequence: N/A
Salt Form: No
Molecular Formula: C₃₃H₃₉N₇O₂
Molecular Weight: 565.72
Cell-Permeable?: True
Purity: ≥98% by HPLC
Solubilities: >40 mg/ml in DMSO
Handling: Do not take internally. Wear gloves and mask when handling the product! Avoid contact by all modes of exposure.
Country of Origin: USA
Tag Line: A potent, selective, and irreversible covalent inhibitor of KRAS G12C
MDL Number:
PubChem CID: 134326100
SMILES: CC1=C2C(=CC=C1)C=CC=C2N3CCC4=C(C3)N=C(N=C4N5CCN(C(C5)CC#N)C(=O)C=C)OCC6CCCN6C
InChi: InChI=1S/C33H39N7O2/c1-4-30(41)40-19-18-39(20-25(40)13-15-34)32-27-14-17-38(29-12-6-10-24-9-5-8-23(2)31(24)29)21-28(27)35-33(36-32)42-22-26-11-7-16-37(26)3/h4-6,8-10,12,25-26H,1,7,11,13-14,16-22H2,2-3H3
InChi Key: YRYQLVCTQFBRLD-UHFFFAOYSA-N