| Identification | Back Directory | [Name]
4-[(3-BROMOPHENYL)AMINO]-6,7-DIETHOXYQUINAZOLINE | [CAS]
171745-13-4 | [Synonyms]
COMPOUND 56
4-[(3-BROMOPHENYL)AMINO]-6,7-DIETHOXYQUINAZOLINE
N-(3-broMophenyl)-6,7-diethoxyquinazolin-4-aMine
N-(3-Bromophenyl)-6,7-diethoxy-4-quinazolinamine
4-Quinazolinamine, N-(3-bromophenyl)-6,7-diethoxy- | [Molecular Formula]
C18H18BrN3O2 | [MDL Number]
MFCD01074974 | [MOL File]
171745-13-4.mol | [Molecular Weight]
388.26 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
insoluble in H2O; ≥16.95 mg/mL in DMSO; ≥47.6 mg/mL in EtOH with ultrasonic | [form ]
White to off-white powder. |
| Hazard Information | Back Directory | [Uses]
Compound 56 is a potent and specific inhibitor of the tyrosine kinase activity of the epidermal growth factor. | [Biological Activity]
compound 56, 4-[(3-bromophenyl)amino]-6,7-diethoxyquinazoline, is a potent and specific inhibitor of the tyrosine kinase of the epidermal growth factor receptor (egfr) showing an ic50 of 0.006 nm. it competitively binds at the adenosine-triphosphate (atp) site of egfr. compound 56 is capable of inhibiting the phosphorylation of egf-dependent egfr, suppressing the proliferation and clonogenicity of a wide panel of egfr-overexpressing human cancer lines, and blocking egf-mediated mitogenesis and oncogenic transformation in fibroblasts overexpressing egfr. besides inhibiting egfr tyrosine kinase, it also inhibits the tyrosine kinase of human epidermal growth factor receptor 2 (her2/neu) but with a less potency.bridges aj, zhou h, cody dr, rewcastle gw, mcmichael a, showalter hd, fry dw, kraker aj, and denny wa. tyrosine kinase inhibitors. 8. an unusually steep structure-activity relationship for analogues of 4-(3-bromoanilino)-6,7-dimethoxyquinazoline (pd 153035), a potent inhibitor of the epidermal growth factor receptor.j med chem 1966; 39 (1): 267-276monique bos, jhn mendelsohn, young-mee kim, joan albanell, david w. fry, and jose baelga. pd153035, a tyrosine kinase inhibitor, prevents epidermal growth factor receptor activation and inhibits growth of cancer cells in a receptor number-dependent manner. clin cancer res 1997;3:2099-2106 | [target]
EGFR |
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