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AZD9291
- Osimertinib
- Soluble in 0.1N HCl(aq) and DMSO
- MF: C28H33N7O2
- MW: 499.61
Description
AZD9291 (Osimertinib) is a potent, irreversible third-generation EGFR tyrosine kinase inhibitor that selectively targets sensitizing and T790M resistance-mutant EGFR while showing lower activity against wild-type EGFR. Reported IC50 values include 1 nM for L858R/T790M, 12 nM for L858R, 5 nM for L861Q and 184 nM for wild-type EGFR.
EGFR resistance mutations, especially T790M, are key mechanisms of acquired resistance in non-small cell lung cancer. AZD9291 is a benchmark tool for studying mutant-selective EGFR inhibition and NSCLC resistance pharmacology.
Key Features
- Third-generation irreversible EGFR TKI
- IC50: 1 nM against L858R/T790M EGFR
- Selects for mutant EGFR over wild-type EGFR
- Targets sensitizing and resistance EGFR mutations
Applications
- EGFR-mutant NSCLC research
- T790M resistance studies
- ERBB kinase pharmacology
- Oncology signaling and proliferation assays
More Information
| Parent CAS No. | 1421373-65-0 |
|---|---|
| Chemical Name | N-(2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxy-5-(4-(1-methyl-1H-indol-3-yl)pyrimidin-2-ylamino)phenyl)acrylamide |
| SMILES | C(NC1=CC(NC2=NC=CC(C3C4=C(N(C)C=3)C=CC=C4)=N2)=C(OC)C=C1N(CCN(C)C)C)(=O)C=C |
| MFCD | N.A. |
| InChi | InChI=1S/C28H33N7O2/c1-7-27(36)30-22-16-23(26(37-6)17-25(22)34(4)15-14-33(2)3)32-28-29-13-12-21(31-28)20-18-35(5)24-11-9-8-10-19(20)24/h7-13,16-18H,1,14-15H2,2-6H3,(H,30,36)(H,29,31,32) |
| InChiKey | DUYJMQONPNNFPI-UHFFFAOYSA-N |
| CID | 71496458 |
| Short Description | EGFR inhibitor |
References
- F.Y. Niu et al. Novel agents and strategies for overcoming EGFR TKIs resistance. Exp Hematol Oncol. 2014 Jan 11;3(1):2. doi: 10.1186/2162-3619-3-2.
- D.A. Cross et al. AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer. Cancer Discov. 2014, 4, 1046-1061
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