CP-724,714

  Cat. No.:  DC8251  
Chemical Structure
383432-38-0
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More than 5000 active chemicals with high quality for research!
Field of application
CP-724,714 is a potent, selective inhibitor of HER2/ErbB2 with IC50 of 10 nM, >640-fold selectivity against EGFR, InsR, IRG-1R, PDGFR, VEGFR2, Abl, Src, c-Met etc. Phase 2.
Cas No.: 383432-38-0
Chemical Name: 2-Methoxy-N-[(2E)-3-[4-[[3-methyl-4-[(6-methyl-3-pyridinyl)oxy]phenyl]amino]-6-quinazolinyl]-2-propen-1-yl]acetamide
Synonyms: CP-724,714,CP724,714,CP 724714,CP 724,714,CP724714,CP-724714
SMILES: O=C(COC)NC/C=C/C1=CC2=C(N=CN=C2C=C1)NC3=CC=C(C(C)=C3)OC4=CC=C(N=C4)C
Formula: C27H27N5O3
M.Wt: 469.54
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: CP-724,714 is a potent, selective inhibitor of HER2/ErbB2 with IC50 of 10 nM, >640-fold selectivity against EGFR, InsR, IRG-1R, PDGFR, VEGFR2, Abl, Src, c-Met etc. Phase 2.in vitro: CP-724,714 is marked selectively against EGFR with IC50 of 6.4 μM. CP-724,714 is >1,000-fold less potent for IR, IGF-1R, PDGFRβ, VGFR2, abl. Src, c-Met c-jun NH2-terminal kinase (JNK)-2, JNK-3, ZAP-70, cyclin-dependent kinase (CDK)-2, and CDK-5. CP-724,714 potently reduces the EGF-induced autophosphorylation of the chimera containing the erbB2 kinase domain with IC50 of 32 nM, but is markedly less potent against EGFR in transfected NIH3T3 cells. CP-724,714 sensitively inhibits the proliferation of erbB2-amplified cells including BT-474 and SKBR3, with IC50 of 0.25 and 0.95 μM. CP-724,714 induces the accumulation of cells in G1 phase and a marked reduction in S-phase in BT-474 cells at 1 μM. CP-724,714 likely exerts its hepatotoxicity via both hepatocellular injury and hepatobiliary cholestatic mechanisms. CP-724,714 displays inhibition of cholyl-lysyl fluorescein and taurocholate (TC) efflux into canaliculi in cryopreserved and fresh cultured human hepatocytes, respectively. CP-724,714 inhibits TC transport in membrane vesicles expressing human bile salt export pump with IC50 of 16 μM and inhibits the major efflux transporter in bile canaliculi, MDR1, with IC50 of ~28 μM. in vivo: CP-724,714 (25 mg/kg) is rapidly absorbed after p.o. administration and causes reduction of tumor erbB2 receptor phosphorylation after dosing in FRE-erbB2 or BT-474 xenografts. CP-724,714 induces apoptosis in FRE-erbB2 xenograft–bearing (s.c.) mice and shows 50% tumor growth inhibition at 50 mg/kg, without weight loss or mortality. CP-724,714 also has great antitumor activity in MDA-MB-453, MDA-MB-231, LoVo (colon), and Colo-205 (colon) xenografts. Furthermore, CP-724,714 (30 or 100 mg/kg) reduces the extracellular signal–regulated kinase and Akt phosphorylation in BT-474 xenografts. For the detailed information of CP-724,714, the solubility of CP-724,714 in water, the solubility of CP-724,714 in DMSO, the solubility of CP-724,714 in PBS buffer, the animal experiment (test) of CP-724,714, the cell expriment (test) of CP-724,714, the in vivo, in vitro and clinical trial test of CP-724,714, the EC50, IC50,and affinity,of CP-724,714, For the detailed information of CP-724,714, the solubility of CP-724,714 in water, the solubility of CP-724,714 in DMSO, the solubility of CP-724,714 in PBS buffer, the animal experiment (test) of CP-724,714, the cell expriment (test) of CP-724,714, the in vivo, in vitro and clinical trial test of CP-724,714, the EC50, IC50,and affinity,of CP-724,714, Please contact DC Chemicals.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
Cat. No. Product name Field of application
DC47250 Nonanal Nonanal is a saturated fatty aldehyde with antidiarrhoeal activity.
DC47249 Piperitone Piperitone is as a powerful repellent and antiappetent agent. Piperitone is very toxic to Cymbopogon schoenanthus (C. schoenanthus) adults, newly laid eggs and to neonate larvae. Insecticidal activity.
DC47247 Tyrosylleucine TFA Tyrosylleucine (Tyr-Leu, YL) TFA, an orally active dipeptide, exhibits a potent antidepressant-like activity.
DC47243 Dehydroglyasperin C Dehydroglyasperin C, a isoflavone, is a potent NAD(P)H:oxidoquinone reductase (NQO1) and phase 2 enzyme inducer. Dehydroglyasperin C has antioxidant, neuroprotective, cancer chemopreventive, and anti-inflammatory activities.
DC47227 (−)-Myrtenal (−)-Myrtenal ((1R)-(−)-Myrtenal) is an orally active terpene with antitumour activity. (−)-Myrtenal ameliorates hyperglycemia by enhancing GLUT2 through Akt in the skeletal muscle and liver of diabetic rats.
DC47224 GPX4-IN-3 GPX4-IN-3 (26a) is a potent glutathione peroxidase 4 (GPX4) inhibitor as a selective ferroptosis inducer. GPX4-IN-3 (26a) exhibits 71.7% inhibition for GPX4 with 1 μM.
DC47179 Tyrosylleucine Tyrosylleucine (Tyr-Leu, YL), an orally active dipeptide, exhibits a potent antidepressant-like activity.
DC47178 Mead acid Mead acid (5,8,11-Eicosatrienoic acid), an unsaturated (Omega-9) fatty acid, is an indicator of essential fatty acid deficiency.
DC47140 Yadanzioside K Yadanzioside K is a natural quassinoid glucoside found in Brucea amarissima.
DC47105 Complanatoside B Complanatoside B is a P. chinense Fisch flavonoid with potential anti-inflammatory effects.
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