CP-724714 succinate
Based on 4 publication(s) in Google Scholar
CP-724714 succinate is an orally active and selective HER2 tyrosine kinase inhibitor with an IC50 of 10 nM. CP-724714 succinate inhibits HER2 receptor autophosphorylation and blocks the downstream Ras-Raf-Mek-Erk signaling pathway, thereby inducing cell cycle arrest and apoptosis in tumor cells. CP-724714 succinate exhibits antiviral activity and inhibits various porcine diarrheal coronaviruses, including SADS-CoV (IC50 of 0.91 μM). CP-724714 succinate is an inhibitor of the hepatic transport receptors OATP1B1/MDR1/BSEP, and can enter hepatocytes via active uptake and trigger the accumulation of drugs and bile acids within hepatocytes. CP-724714 succinate can be used in research related to HER2-overexpressing breast cancer and porcine diarrheal coronavirus infection.
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- CAS. Nr.: 543681-31-8
- Formel: C27H27N5O3·3/2C4H6O4
- Molecular Weight:646.68
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Publications Citing Use of MedChemExpress (MCE) CP-724714 succinate
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
HER2 10 nM (IC50) |
ERK1 |
ERK2 |
RAF |
In Vitro
CP-724714 (10-40 µM) succinate shows no significant effect on the viability of Vero cells and IPI-21 cells, and dose-dependently inhibits SADS-CoV infection[1].
CP-724714 (20-30 µM; 12 h) succinate exhibits anti-SADS-CoV activity targeting the viral infection replication stage in IPI-21 cells and reduces HER2, Raf, and Erk phosphorylation[1].
CP-724714 (12 h) succinate exhibits broad-spectrum anti-porcine diarrheal coronavirus (SADS-CoV, PEDV, PDCoV, and TGEV) activity in Vero cells and ST cells, with IC50 values of 0.91, 2.13, 0.84, and 2.53 μM, respectively[1].
CP-724714 (up to 10 µM; 2 h) succinate potently inhibits EGF-induced EGFR/erbB2 chimera autophosphorylation in NIH 3T3 transfected cells with an IC50 of 32 nM, while showing minimal effect on EGFR autophosphorylation in EGFR-transfected NIH 3T3 cells[2].
CP-724,714 (0.03-3 μM; 6 days) succinate reduces colony formation in erbB2-overexpressing human breast cancer cells BT-474 and SKBR3[2].
CP-724714 (1 μM; 24 h) succinate induces G1 phase cell cycle arrest and reduces S phase cells in human breast cancer BT-474 cells[2].
CP-724714 (24 h) succinate exerts a direct cytotoxic effect that decreases mitochondrial membrane potential in human primary hepatocytes[3].
CP-724714 succinate potently inhibits recombinant erbB2 kinase with an IC50 of 10 nM[2].
CP-724714 (1.2-100 µM; 7 min) succinate inhibits BSEP-mediated taurocholate (TC) transport in membrane vesicles expressing human BSEP, with an IC50 of 16 µM[3].
CP-724714 (2 µM; up to 120 min) succinate is rapidly taken up and excreted into the canaliculi in sandwich-cultured human hepatocytes[3].
CP-724714 (0.01-100 µM; 5 min) succinate concentration-dependently inhibits OATP1B1-mediated substrate uptake in OATP1B1-transfected HEK 293 cells with an IC50 of 1.7 µM[3].
CP-724714 (0.3-100 µM) succinate inhibits MDR1-mediated efflux transport of substrate in MDR1-transfected MDCK cells with an IC50 of approximately 28 µM[3].
CP-724714 (10-100 µM; 15 min) succinate concentration-dependently inhibits CLF (IC50 approximately 5 µM) and TC efflux into canaliculi in sandwich-cultured fresh and cryopreserved human hepatocytes[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BT-474 cells
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Concentration:1 µM
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Incubation Time:24 h
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Result:Caused an accumulation of cells in the G1 phase and a marked reduction of cells in the S-phase.
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Cell Line:BT-474 cells and SKBR3 cells
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Concentration:0.03, 0.3, 1, 3 µM
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Incubation Time:6 days
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Result:Reduced colony formation by >80% leading to cell death.
In Vivo
CP-724714 (25 mg/kg; p.o.; single administration; 0.5-8 h) succinate is rapidly absorbed and leads to decreased phosphorylation of the tumor erbB2 receptor in athymic female mouse models bearing FRE-erbB2 xenografts[2].
CP-724714 (6.25-100 mg/kg; p.o.; once daily; for 8 consecutive days) succinate exhibits activity in inhibiting xenograft growth in athymic female mouse models bearing FRE-erbB2 xenografts[2].
CP-724714 (1-100 mg/kg; p.o.; twice daily; 40 days) succinate exhibits dose-dependent inhibition of tumor growth and causes tumor regression at high doses in athymic female mouse models bearing human breast cancer BT-474 xenografts[2].
CP-724714 (25-100 mg/kg; p.o.; twice daily; 48 days) succinate significantly inhibits tumor growth in athymic female mouse models bearing human breast cancer MDA-MB-453 xenografts[2].
CP-724714 (30-100 mg/kg; p.o.; single administration; 0.5 h) succinate significantly decreases the levels of activated Erk and Akt phosphorylation in tumors in athymic female mouse models bearing BT-474 xenografts[2].
CP-724714 (30-100 mg/kg; p.o.; single administration; 0.5-8 h) succinate induces time- and dose-dependent tumor cell apoptosis and increases cleaved caspase-3 release in athymic female mouse models bearing FRE-erbB2 xenografts[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CD-1 nu/nu (female, ~20 g, FRE-erbB2 fibroblast xenograft model)[2]
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Dosage:3.125, 6.25, 12.5, 25, 30, 50, 100 mg/kg
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Administration:p.o.; single dose or once daily; processed from 0.5 to 8 hours for pharmacodynamic evaluation, or dosed for 8 consecutive days for tumor growth
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Result:Reduced the phosphorylation of erbB2 receptors in the tumors.
Induced apoptosis of tumor cells and increased the immunostaining for cleaved caspase-3.
Inhibited the growth of FRE-erbB2 xenografts in a dose-dependent manner.
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Animal Model:CD-1 nu/nu (female, ~20 g, BT-474 or MDA-MB-231 human breast carcinoma xenograft model)[2]
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Dosage:1, 10, 25, 30, 50, 100 mg/kg
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Administration:p.o.; twice daily or single dose; dosed for up to 40 or 48 consecutive days, or evaluated at 0.5 hours for signaling
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Result:Inhibited the growth of human breast carcinoma xenografts (BT-474 and MDA-MB-453) dose-dependently, leading to tumor regression at the highest dose in the BT-474 model.
Markedly reduced the levels of phosphorylated Erk and phosphorylated Akt in BT-474 xenografts within 0.5 hours of administration.
- Research Protocol for Infectious Diseases
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Flow cytometric DNA-content cell-cycle staining
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- Apoptosis Solutions
- Protocol for Cell Cycle
- Breast Cancer Modeling
Chemical Information
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CAS. Nr. 543681-31-8
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Molecular Weight 646.68
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Formel C27H27N5O3·3/2C4H6O4
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SMILES
OC(CCC(O)=O)=O.COCC(NC/C=C/C1=CC(C(NC2=CC(C)=C(C=C2)OC3=CN=C(C)C=C3)=NC=N4)=C4C=C1)=O.[1.5]
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (4)
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Journal Impact Factor
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Most Recent
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Cell Host Microbe
Peptostreptococcus stomatis promotes colonic tumorigenesis and receptor tyrosine kinase inhibitor resistance by activating ERBB2-MAPK. [Abstract]2024 Aug 14;32(8):1365-1379.e10. PMID: 39059397 -
Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
Virol Sin
Identification of a receptor tyrosine kinase inhibitor CP-724714 inhibits SADS-CoV related swine diarrhea coronaviruses infection in vitro. [Abstract]2023 Oct;38(5):778-786. PMID: 37406816
Reinheit & Dokumentation
Verweise
[1]. Zhou L, et al. Identification of a receptor tyrosine kinase inhibitor CP-724714 inhibits SADS-CoV related swine diarrhea coronaviruses infection in vitro. Virologica Sinica. 2023 Oct;38(5):778-786. [Content Brief]
[2]. Jani JP, et al. Discovery and pharmacologic characterization of CP-724,714, a selective ErbB2 tyrosine kinase inhibitor. Cancer research. 2007 Oct 15;67(20):9887-93. [Content Brief]
[3]. Feng B, et al. Role of hepatic transporters in the disposition and hepatotoxicity of a HER2 tyrosine kinase inhibitor CP-724,714. Toxicological sciences : an official journal of the Society of Toxicology. 2009 Apr;108(2):492-500. [Content Brief]
Calculators
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