-Ethyl (3-(4-((3-methyl-4-((6-methylpyridin-3-yl)
CP-724714
CAS: 537705-08-1
Molecular Formula: C27H27N5O3
-Ethyl (3-(4-((3-methyl-4-((6-methylpyridin-3-yl) - Names and Identifiers
-Ethyl (3-(4-((3-methyl-4-((6-methylpyridin-3-yl) - Physico-chemical Properties
| Molecular Formula | C27H27N5O3 |
| Molar Mass | 469.54 |
| Solubility | DMSO 94 mg/mL Water <1 mg/mL Ethanol 94 mg/mL |
| Storage Condition | -20℃ |
| Use | Marked selectively against EGFR and potently reduces the EGF-induced autophosphorylation. |
| In vitro study | CP-724,714 was significantly selective for EGFR,IC50 was 6.4 M. CP-724,714 acts on IR,IGF-1R,PDGFR β,VGFR2,Abl,Src,c-Met,c-jun NH2-terminal kinase (JNK)-2,JNK-3,ZAP-70, cyclin-dependent kinase (Cdk)-2, and Cdk-5 were more than 1000-fold less effective. CP-724,714 acts on the chimera containing erbB2 kinase domain, effectively reducing EGF induced autophosphorylation, IC50 is 32 nM, but the effect on NIH3T3 cells transfected with EGFR is significantly lower. CP-724,714 inhibited the proliferation of erbB2 enhanced cells, including BT-474 and SKBR3, with IC50 of 0.25 and 0.95 μm, respectively. 1 M CP-724,714 in BT-474 cells, induced cell accumulation in the G1 phase, while in the S phase was significantly reduced. CP-724,714 may show hepatotoxicity through the mechanism of hepatocellular injury and cholestasis. CP-724,714 inhibition of Taurocholic acid (TC) into the expression of human bile salt export pump membrane vesicles, IC50 16 μm, and inhibit the bile tubule, the main efflux of MDR1 transport, the IC50 was ~ 28 μm. |
| In vivo study | CP-724,714 at a dose of 25 mg/kg oral treatment of FRE-erbB2 and BT-474 transplanted tumor, rapid absorption, and cause the tumor erbB2 receptor phosphorylation decreased. On CP-724,714 induced apoptosis in mice injected subcutaneously with FRE-erbB2 xenografts. Treatment at a dose of 50 mg/kg showed tumor growth inhibition of 50% and did not cause weight loss or death. CP-724,714 acts on MDA-MB-453,MDA-MB-231,LoVo (colon), and Colo-205 (colon) transplanted tumors with strong anticancer activity. Furthermore, CP-724,714 treatment of BT-474 of xenografts at 30 or 100 mg/kg dose reduced extracellular signal-regulated kinase and Akt phosphorylation. |
-Ethyl (3-(4-((3-methyl-4-((6-methylpyridin-3-yl) - Introduction
CP-724714 is an effective and selective HER2/ErbB2 inhibitor with IC50 of 10 nM, which is more than 640 times higher than EGFR, InsR, IRG-1R, PDGFR, VEGFR2, Abl, Src, c-Met, etc.
Last Update：2022-10-16 17:41:42
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Product Name: CP-724714 Visit Supplier Webpage Request for quotation
CAS: 537705-08-1
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 537705-08-1
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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