MRTX1257
Axon 3733
CAS:
2206736-04-9
- Optical Purity: 99% d.e.
- Soluble in DMSO
- MF: C33H39N7O2
- MW: 565.71
Description
MRTX1257 is an orally available, potent, selective, and irreversible covalent inhibitor of KRAS G12C. It inhibits KRAS dependent ERK-phosphorylation in the H358 cell with IC50 of 0.9 nM, and is highly selective for the Cys12 of KRAS G12C in NCI-H358 cells over other cysteines; Demonstrates robust target engagement in vivo; Exhibits rapid and sustained efficacy against MIA PaCa-2 Xenocrafts, in which, at 100 mg/kg daily dose, leads to complete responses that are maintained >70 days after cessation of treatment.
More Information
| Parent CAS No. | 2206736-04-9 |
|---|---|
| Chemical Name | 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 |
| extra_info | Sold in collaboration with Chemietek |
| SMILES | C12CCN(C3C4C(C)=CC=CC=4C=CC=3)CC=1N=C(OC[C@@H]1CCCN1C)N=C2N1C[C@H](CC#N)N(C(=O)C=C)CC1 |&1:21,31,r| |
| MFCD | N.A. |
| 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/t25-,26-/m0/s1 |
| InChiKey | YRYQLVCTQFBRLD-UIOOFZCWSA-N |
| CID | 134326084 |
| Short Description | KRAS-G12C inhibitor |
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