| Identification | Back Directory | [Name]
2-Butenamide, N-[4-[(3-chloro-2-fluorophenyl)amino]-7-[2-[(1R,5S)-3-methyl-3-azabicyclo[3.1.0]hex-1-yl]ethynyl]-6-quinazolinyl]-4-(4-morpholinyl)-, (2E)- | [CAS]
2607829-38-7 | [Synonyms]
BDTX-1535
2-Butenamide, N-[4-[(3-chloro-2-fluorophenyl)amino]-7-[2-[(1R,5S)-3-methyl-3-azabicyclo[3.1.0]hex-1-yl]ethynyl]-6-quinazolinyl]-4-(4-morpholinyl)-, (2E)- | [Molecular Formula]
C30H30ClFN6O2 | [MOL File]
2607829-38-7.mol | [Molecular Weight]
561.05 |
| Chemical Properties | Back Directory | [Boiling point ]
730.0±60.0 °C(Predicted) | [density ]
1.42±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
11.44±0.43(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
BDTX-1535 (EGFR-IN-76, compound 37A) is an orally active, brain-penetrant, selective and potent EGFR tyrosine kinase inhibitor. BDTX-1535 achieves potent anti-tumor activity against EGFR alterations and amplification across models including NSCLC, GBM PDX and intracranial tumors[1][2][3]. | [References]
[1] Lucas MC, et al. Preparation of alkynyl quinazoline compounds as anticancer agents. World Intellectual Property Organization, WO2021030711 A1. 2021-02-18.
[2] O'Connor M, et al. Discovery of BDTX-1535, a novel 4th generation, irreversible, potent, wild type sparing EGFR MasterKey inhibitor that targets oncogenic kinase domain mutations as well as extracellular domain alterations for the treatment of NSCLC and GBM[J]. Cancer Research, 2023, 83(7_Supplement): 3396-3396.
[3] Lucas M, et al. BDTX-1535, a fourth generation EGFR inhibitor, targeting intrinsic and acquired resistance mutations in NSCLC[J]. European Journal of Cancer, 2022, 174: S22. |
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