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537705-08-1

537705-08-1 Structure

537705-08-1 Structure
IdentificationBack Directory
[Name]

CP-724714
[CAS]

537705-08-1
[Synonyms]

CS-521
CS-2401
CP-724714
(E/Z)-CP-724714
CP-724714 USP/EP/BP
-Ethyl (3-(4-((3-methyl-4-((6-methylpyridin-3-yl)
(E)-Ethyl (3-(4-((3-methyl-4-((6-methylpyridin-3-yl)-oxy)phenyl)amino)quinazolin-6-yl)allyl)ca
(E)-Ethyl (3-(4-((3-methyl-4-((6-methylpyridin-3-yl)-oxy)phenyl)amino)quinazolin-6-yl)allyl)carba
(E)-Ethyl (3-(4-((3-Methyl-4-((6-Methylpyridin-3-yl)oxy)phenyl)aMino)quinazolin-6-yl)allyl)carbaMate
(E)-2-Methoxy-N-(3-(4-(3-Methyl-4-(6-Methylpyridin-3-yloxy)phenylaMino)quinazolin-6-yl)allyl)acetaMide
2-Methoxy-N-[3-[4-[[3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino]quinazolin-6-yl]allyl]acetamide
2-Methoxy-N-[3-[4-[[3-methyl-4-[(6-methyl-3-pyridinyl)oxy]phenyl]amino]-6-quinazolinyl]-2-propen-1-yl]acetamide
acetaMide, 2-Methoxy-N-[3-[4-[[3-Methyl-4-[(6-Methyl-3-pyridinyl)oxy]phenyl]aMino]-6-quinazolinyl]-2-propen-1-yl]-
[Molecular Formula]

C27H27N5O3
[MDL Number]

MFCD19687281
[MOL File]

537705-08-1.mol
[Molecular Weight]

469.54
Chemical PropertiesBack Directory
[solubility ]

≥23.5 mg/mL in DMSO; insoluble in H2O; ≥25.4 mg/mL in EtOH
[form ]

solid
Hazard InformationBack Directory
[Uses]

CP-724,714 is a potent, selective inhibitor of HER2/ErbB2 with IC50 of 10 nM and also inhibits EGFR with IC50 of 6.4 μM.
[Biological Activity]

cp-724714 is an inhibitor of erbb2 and egfr kinases with ic50 values of 10±3 nmol/l and 6,400±2,100 nmol/l, respectively [1].in the in vitro cell cycle assay, cp-724714 cause a g1 block of the her2-amplified bt-474 breast cancer cells due to its inhibition of erbb2. cp-724714 at 1 ?mol/l can also reduce the level of phospho-erbb2 in these cells. in in vivo assay, cp-724714 cause a concentration-dependent reduction of tumor erbb2 receptor phosphorylation in athymic mice bearing fre-erbb2xenografts. cp-724714 treatments also resulted in a time- and dose-dependent induction of tumor cell apoptosis. in two human breast carcinoma models, bt-474 and mda-mb-453, which are her2 amplified and highly overexpress erbb2, cp-724714 is found to produce a dose-dependent inhibition of xenograft growth. in addition, cp-724,714 treatments induce reduction of downstream erbb2 rtk signaling. on the basis of these, cp-724,714 was advanced to phase i
[target]

erbB2
[IC 50]

HER2
[References]

[1] jitesh p. jani, richard s. finn, mary campbell, et al. discovery and pharmacologic characterization of cp-724714, a selective erbb2 tyrosine kinase inhibitor. cancer research. 2007 (67): 9887-9893.
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