CP-724714
Synonym(s):(E)-2-Methoxy-N-[3-[4-[[3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino]quinazolin-6-yl]allyl]ethanamide;2-Methoxy-N-[(2E)-3-[4-[[3-methyl-4-[(6-methyl-3-pyridinyl)oxy]phenyl]amino]-6-quinazolinyl]-2-propen-1-yl]-acetamide;CP-724,714;CP-724714
- CAS NO.:537705-08-1
- Empirical Formula: C27H27N5O3
- Molecular Weight: 469.54
- MDL number: MFCD19687281
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-11-19 23:02:33
What is CP-724714?
The Uses of CP-724714
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.
What are the applications of Application
CP-724714 is marked selectively against EGFR and potently reduces the EGF-induced autophosphorylation
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].
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.
Properties of CP-724714
solubility | ≥23.5 mg/mL in DMSO; insoluble in H2O; ≥25.4 mg/mL in EtOH |
form | solid |
Safety information for CP-724714
Computed Descriptors for CP-724714
New Products
4-AMINO-TETRAHYDRO-PYRAN-4-CARBOXYLIC ACID HCL 4-(Dimethylamino)tetrahydro-2H-pyran-4-carbonitrile 4-AMINO-TETRAHYDRO-PYRAN-4-CARBOXYLIC ACID 4-Aminotetrahydropyran-4-carbonitrile Hydrochloride (R)-3-Aminobutanenitrile Hydrochloride 5-Bromo-2-nitropyridine Nimesulide BP Aceclofenac IP/BP/EP Diclofenac Sodium IP/BP/EP/USP Mefenamic Acid IP/BP/EP/USP Ornidazole IP Diclofenac Potassium 3-Bromopyrazole (3aR,4R,5R,6aS)-hexahydro-5-Triethyl silyloxy-4-((E)-3-oxo-5-phenylpent-1- enyl)cyclopenta[b]furan-2-one. 1-Chlorocarbonyl-4-piperidinopiperidine 1-Bromo-4-phenyl-2-Butanone 4-Amino-2-fluoro-N-methylbenzamide 1,1'-Carbonyldiimidazole SODIUM AAS SOLUTION ZINC AAS SOLUTION BUFFER SOLUTION PH 10.0(BORATE) GOOCH CRUCIBLE SINTERED AQUANIL 5 BERYLLIUM AAS SOLUTIONRelated products of tetrahydrofuran
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