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MRTX1133
Axon 3761
CAS:
2621928-55-8
- Optical Purity: 0.99
- Soluble in DMSO
- MF: C33H31F3N6O2
- MW: 600.63
Description
MRTX1133 is a first-in-class, noncovalent, selective & reversible inhibitor of KRASG12D mutant in both active and inactive states. Demonstrates selective inhibition of cell viability of KRASG12D mutant, but not KRAS wild-type, tumor cells. Displays sustained dose-dependent inhibition of KRAS-dependent signaling in mouse tumor models.
More Information
| Parent CAS No. | 2621928-55-8 |
|---|---|
| Chemical Name | 4-(4-(3,8-Diazabicyclo[3.2.1]octan-3-yl)-8-fluoro-2-(((2R,7aS)-2-fluorohexahydro-1H-pyrrolizin-7a-yl)methoxy)pyrido[4,3-d]pyrimidin-7-yl)-5-ethynyl-6-fluoronaphthalen-2-ol |
| SMILES | N1C=C2C(N3CC4NC(CC4)C3)=NC(OC[C@]34C[C@@H](F)CN3CCC4)=NC2=C(F)C=1C1C=C(O)C=C2C=CC(F)=C(C#C)C=12 |&1:16,18,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C33H31F3N6O2/c1-2-23-26(35)7-4-18-10-22(43)11-24(27(18)23)29-28(36)30-25(13-37-29)31(41-15-20-5-6-21(16-41)38-20)40-32(39-30)44-17-33-8-3-9-42(33)14-19(34)12-33/h1,4,7,10-11,13,19-21,38,43H,3,5-6,8-9,12,14-17H2/t19-,20?,21?,33+/m1/s1 |
| InChiKey | SCLLZBIBSFTLIN-IFMUVJFISA-N |
| CID | 156124857 |
| Short Description | KRASG12D mutant inhibitor |
References
- D Sun et al. Discovery of AMG 232, a Potent, Selective, and Orally Bioavailable MDM2–p53 Inhibitor in Clinical Development. J. Med. Chem., 2014, 57, 1454–1472.
- J Canon et al. The MDM2 Inhibitor AMG 232 Demonstrates Robust Antitumor Efficacy and Potentiates the Activity of p53-Inducing Cytotoxic Agents. Mol Cancer Ther. 2015 Mar, 14(3), 649-58.
- Y. Rew. et al. Discovery of a small molecule MDM2 inhibitor (AMG 232) for treating cancer. J Med Chem. 2014 Aug 14, 57(15), 6332-41.
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