CP-724714
Based on 4 publication(s) in Google Scholar
CP-724714 is an orally active and selective HER2 tyrosine kinase inhibitor with an IC50 of 10 nM. CP-724714 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 exhibits antiviral activity and inhibits various porcine diarrheal coronaviruses, including SADS-CoV (IC50 of 0.91 μM). CP-724714 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 can be used in research related to HER2-overexpressing breast cancer and porcine diarrheal coronavirus infection.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté : 98.72%
- CAS No.: 383432-38-0
- Formule: C27H27N5O3
- Masse moléculaire:469.55
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) CP-724714
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Activité biologique
Description
IC50 & Target
[1]|
HER2 10 nM (IC50) |
ERK1 |
ERK2 |
RAF |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BT-20 | IC50 |
>10 μM
Compound: Chemical Probe: CP-724,714
|
Antiproliferative activity against human BT-20 cells assessed as inhibition of cell growth
Antiproliferative activity against human BT-20 cells assessed as inhibition of cell growth
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[PMID: 17942920] |
| BT-474 | EC50 |
0.77 μg/mL
Compound: Chemical Probe: CP-724,714
|
Antitumor activity against human BT-474-erbB2 cells xenografted bearing female athymic nu-nu CD-1 mouse assessed as reduction in tumor erbB2 receptor phosphorylation, po administration by ELISA method
Antitumor activity against human BT-474-erbB2 cells xenografted bearing female athymic nu-nu CD-1 mouse assessed as reduction in tumor erbB2 receptor phosphorylation, po administration by ELISA method
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[PMID: 17942920] |
| BT-474 | IC50 |
0.25 μM
Compound: Chemical Probe: CP-724,714
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Antiproliferative activity against human BT-474 cells assessed as inhibition of cell growth
Antiproliferative activity against human BT-474 cells assessed as inhibition of cell growth
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[PMID: 17942920] |
| CAMA-1 | IC50 |
>10 μM
Compound: Chemical Probe: CP-724,714
|
Antiproliferative activity against human CAMA-1 cells assessed as inhibition of cell growth
Antiproliferative activity against human CAMA-1 cells assessed as inhibition of cell growth
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[PMID: 17942920] |
| EFM-19 | IC50 |
>10 μM
Compound: Chemical Probe: CP-724,714
|
Antiproliferative activity against human EFM-19 cells assessed as inhibition of cell growth
Antiproliferative activity against human EFM-19 cells assessed as inhibition of cell growth
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[PMID: 17942920] |
| HCC1419 | IC50 |
1 μM
Compound: Chemical Probe: CP-724,714
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Antiproliferative activity against human HCC1419 cells assessed as inhibition of cell growth
Antiproliferative activity against human HCC1419 cells assessed as inhibition of cell growth
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[PMID: 17942920] |
| MCF7 | IC50 |
9.8 μM
Compound: Chemical Probe: CP-724,714
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Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth
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[PMID: 17942920] |
| MDA-MB-157 | IC50 |
>10 μM
Compound: Chemical Probe: CP-724,714
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Antiproliferative activity against human MDA-MB-157 cells assessed as inhibition of cell growth
Antiproliferative activity against human MDA-MB-157 cells assessed as inhibition of cell growth
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[PMID: 17942920] |
| MDA-MB-175-VII | IC50 |
0.81 μM
Compound: Chemical Probe: CP-724,714
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Antiproliferative activity against human MDA-MB-175-VII cells assessed as inhibition of cell growth
Antiproliferative activity against human MDA-MB-175-VII cells assessed as inhibition of cell growth
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[PMID: 17942920] |
| MDA-MB-361 | IC50 |
3.7 μM
Compound: Chemical Probe: CP-724,714
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Antiproliferative activity against human MDA-MB-361 cells assessed as inhibition of cell growth
Antiproliferative activity against human MDA-MB-361 cells assessed as inhibition of cell growth
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[PMID: 17942920] |
| MDA-MB-453 | IC50 |
2.5 μM
Compound: Chemical Probe: CP-724,714
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Antiproliferative activity against human MDA-MB-453 cells assessed as inhibition of cell growth
Antiproliferative activity against human MDA-MB-453 cells assessed as inhibition of cell growth
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[PMID: 17942920] |
| MDA-MB-468 | IC50 |
>10 μM
Compound: Chemical Probe: CP-724,714
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Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell growth
Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell growth
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[PMID: 17942920] |
| Sf9 | IC50 |
10 nM
Compound: 37; CP-724714
|
Inhibition of recombinant GST-tagged HER2 (unknown origin) (catalytic domain 675 to 1225) residues expressed in baculovirus-infected Sf9 cells assessed as reduction of phosphorylation of polyglutamic acid/tyrosine incubated for 25 mins by spectrometery
Inhibition of recombinant GST-tagged HER2 (unknown origin) (catalytic domain 675 to 1225) residues expressed in baculovirus-infected Sf9 cells assessed as reduction of phosphorylation of polyglutamic acid/tyrosine incubated for 25 mins by spectrometery
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[PMID: 30878832] |
| SK-BR-3 | IC50 |
0.95 μM
Compound: Chemical Probe: CP-724,714
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Antiproliferative activity against human SK-BR-3 cells assessed as inhibition of cell growth
Antiproliferative activity against human SK-BR-3 cells assessed as inhibition of cell growth
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[PMID: 17942920] |
| T47D | IC50 |
2.4 μM
Compound: Chemical Probe: CP-724,714
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Antiproliferative activity against human T47D cells assessed as inhibition of cell growth
Antiproliferative activity against human T47D cells assessed as inhibition of cell growth
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[PMID: 17942920] |
| UACC-812 | IC50 |
1.9 μM
Compound: Chemical Probe: CP-724,714
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Antiproliferative activity against human UACC-812 cells assessed as inhibition of cell growth
Antiproliferative activity against human UACC-812 cells assessed as inhibition of cell growth
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[PMID: 17942920] |
| ZR-75-1 | IC50 |
>10 μM
Compound: Chemical Probe: CP-724,714
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Antiproliferative activity against human ZR-75-1 cells assessed as inhibition of cell growth
Antiproliferative activity against human ZR-75-1 cells assessed as inhibition of cell growth
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[PMID: 17942920] |
| ZR-75-30 | IC50 |
1.5 μM
Compound: Chemical Probe: CP-724,714
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Antiproliferative activity against human ZR-75-30 cells assessed as inhibition of cell growth
Antiproliferative activity against human ZR-75-30 cells assessed as inhibition of cell growth
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[PMID: 17942920] |
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 No. 383432-38-0
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Appearance Solid
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Masse moléculaire 469.55
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Formule C27H27N5O3
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Color Light yellow to yellow
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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
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
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
Solvant et solubilité
In Vitro:
DMSO : ≥ 50 mg/mL (106.48 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.32 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.32 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (288 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Instruction de manipulation (2659 KB)
Références
[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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1297 mL | 10.6485 mL | 21.2970 mL | 53.2425 mL |
| 5 mM | 0.4259 mL | 2.1297 mL | 4.2594 mL | 10.6485 mL | |
| 10 mM | 0.2130 mL | 1.0648 mL | 2.1297 mL | 5.3242 mL | |
| 15 mM | 0.1420 mL | 0.7099 mL | 1.4198 mL | 3.5495 mL | |
| 20 mM | 0.1065 mL | 0.5324 mL | 1.0648 mL | 2.6621 mL | |
| 25 mM | 0.0852 mL | 0.4259 mL | 0.8519 mL | 2.1297 mL | |
| 30 mM | 0.0710 mL | 0.3549 mL | 0.7099 mL | 1.7747 mL | |
| 40 mM | 0.0532 mL | 0.2662 mL | 0.5324 mL | 1.3311 mL | |
| 50 mM | 0.0426 mL | 0.2130 mL | 0.4259 mL | 1.0648 mL | |
| 60 mM | 0.0355 mL | 0.1775 mL | 0.3549 mL | 0.8874 mL | |
| 80 mM | 0.0266 mL | 0.1331 mL | 0.2662 mL | 0.6655 mL | |
| 100 mM | 0.0213 mL | 0.1065 mL | 0.2130 mL | 0.5324 mL |
CP-724714 Related Classifications
HY-14674 Related Classifications
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