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A potent, selective, and irreversible covalent inhibitor of KRAS G12C
Catalog #: B2614
SKU-Size Size Price Qty
B2614-1 1 mg
B2614-5 5 mg
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Product Details

Alternate Name 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
CAS # 2206736-04-9
Molecular Formula C₃₃H₃₉N₇O₂
Molecular Weight 565.72
Purity ≥98% by HPLC
Solubility >40 mg/ml in DMSO
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
PubChem CID 134326100
Handling Do not take internally. Wear gloves and mask when handling the product! Avoid contact by all modes of exposure.
Storage Conditions -20°C
Shipping Conditions Gel Pack
USAGE For Research Use Only! Not For Use in Humans.


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.

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