CP-724714
CP-724714 Basic information
- Product Name:
- CP-724714
- Synonyms:
-
- (E)-Ethyl (3-(4-((3-Methyl-4-((6-Methylpyridin-3-yl)oxy)phenyl)aMino)quinazolin-6-yl)allyl)carbaMate
- acetaMide, 2-Methoxy-N-[3-[4-[[3-Methyl-4-[(6-Methyl-3-pyridinyl)oxy]phenyl]aMino]-6-quinazolinyl]-2-propen-1-yl]-
- (E)-Ethyl (3-(4-((3-methyl-4-((6-methylpyridin-3-yl)-oxy)phenyl)amino)quinazolin-6-yl)allyl)carba
- CP-724714
- 2-Methoxy-N-[3-[4-[[3-methyl-4-[(6-methyl-3-pyridinyl)oxy]phenyl]amino]-6-quinazolinyl]-2-propen-1-yl]acetamide
- (E)-2-Methoxy-N-(3-(4-(3-Methyl-4-(6-Methylpyridin-3-yloxy)phenylaMino)quinazolin-6-yl)allyl)acetaMide
- -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
- CAS:
- 537705-08-1
- MF:
- C27H27N5O3
- MW:
- 469.54
- Product Categories:
-
- Inhibitors
- Mol File:
- 537705-08-1.mol
CP-724714 Chemical Properties
- solubility
- ≥23.5 mg/mL in DMSO; insoluble in H2O; ≥25.4 mg/mL in EtOH
- form
- solid
CP-724714 Usage And Synthesis
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 clinical trials and is potentially another option for her2-driven breast cancer [1].
target
erbB2
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.
CP-724714Supplier
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