Art. -Nr.: HY-14674

CP-724714

4 Cited Publications

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Based on 4 publication(s) in Google Scholar

CP-724714 is a potent, selective and orally active ErbB2 (HER2) tyrosine kinase inhibitor, with an IC₅₀ of 10 nM. CP-724714 displays a marked selectivity against EGFR kinase (IC₅₀=6400 nM). CP-724714 potently inhibits ErbB2 receptor autophosphorylation in intact cells. Antitumor activities.

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Reinheit: 98.72%
CAS. Nr.: 383432-38-0
Formel: C₂₇H₂₇N₅O₃
Molecular Weight:469.55

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

CP-724714 Chemical Structure

CAS. Nr.: 383432-38-0

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (4)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

ErbB2

10 nM (IC₅₀)

Alle EGFR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	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	[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	[PMID: 17942920]
BT-474	IC₅₀	0.25 μM Compound: Chemical Probe: CP-724,714	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	[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	[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	[PMID: 17942920]
HCC1419	IC₅₀	1 μM Compound: Chemical Probe: CP-724,714	Antiproliferative activity against human HCC1419 cells assessed as inhibition of cell growth Antiproliferative activity against human HCC1419 cells assessed as inhibition of cell growth	[PMID: 17942920]
MCF7	IC₅₀	9.8 μM Compound: Chemical Probe: CP-724,714	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth	[PMID: 17942920]
MDA-MB-157	IC₅₀	>10 μM Compound: Chemical Probe: CP-724,714	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	[PMID: 17942920]
MDA-MB-175-VII	IC₅₀	0.81 μM Compound: Chemical Probe: CP-724,714	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	[PMID: 17942920]
MDA-MB-361	IC₅₀	3.7 μM Compound: Chemical Probe: CP-724,714	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	[PMID: 17942920]
MDA-MB-453	IC₅₀	2.5 μM Compound: Chemical Probe: CP-724,714	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	[PMID: 17942920]
MDA-MB-468	IC₅₀	>10 μM Compound: Chemical Probe: CP-724,714	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	[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	[PMID: 30878832]
SK-BR-3	IC₅₀	0.95 μM Compound: Chemical Probe: CP-724,714	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	[PMID: 17942920]
T47D	IC₅₀	2.4 μM Compound: Chemical Probe: CP-724,714	Antiproliferative activity against human T47D cells assessed as inhibition of cell growth Antiproliferative activity against human T47D cells assessed as inhibition of cell growth	[PMID: 17942920]
UACC-812	IC₅₀	1.9 μM Compound: Chemical Probe: CP-724,714	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	[PMID: 17942920]
ZR-75-1	IC₅₀	>10 μM Compound: Chemical Probe: CP-724,714	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	[PMID: 17942920]
ZR-75-30	IC₅₀	1.5 μM Compound: Chemical Probe: CP-724,714	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	[PMID: 17942920]

In Vitro

CP-724714 is >1,000-fold less potent for insulin receptor, insulin-like growth factor-I receptor, platelet-derived growth factor β, vascular endothelial growth factor 2, Abl, Src, c-Met, JNK-2, JNK-3, ZAP-70, Cdk-2, and Cdk-5^[1].
CP-724714 potently reduces the EGF-induced autophosphorylation of the chimera containing the erbB2 kinase domain at a concentration as low as 50 nmol/L (IC₅₀=32 nM) but is markedly less potent against EGFR^[1].
CP-724714 (1 μM; 24 hours) induces G1 cell cycle block in vitro in erbB2-overexpressing BT-474 human breast carcinoma cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis^[1]

Cell Line:

erbB2-amplified BT-474 breast cancer cells
Concentration:

1 μM
Incubation Time:

24 hours
Result:

Resulted in accumulation of cells in G1 phase and a marked reduction in S-phase cells.

In Vivo

CP-724714 (3.25-100 mg/kg; p.o.; 0.5-8 hours) results in a concentration-dependent reduction of ErbB2 receptor phosphorylation^[1].
CP-724714 (6.25-100 mg/kg; p.o.; q.d; for 8 to 40 day) inhibits FRE-erbB2 xenograft growth^[1].
CP-724714 (Athymic, female FRE-erbB2 xenograft-bearing mice; 30 or 100 mg/kg; p.o.) treatments results in a time- and dose- dependent induction of apoptosis, which was evident as early as 4 to 8 h after dosing. Approximately 75% more tumor cells exhibited apoptotic changes in the 100 mg/kg treatment group compared with vehicle control group at 8 h after dosing. CP-724714 induces regression of BT-474 tumors and significant inhibition in a number of other human tumor xenografts. Additionally, CP-724714 showed a favorable nonclinical toxicity profile with no apparent effects on cardiac tissue^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Female athymic mice (bearing FRE-erbB2 xenografts)^[1]
Dosage:

3.25-100 mg/kg
Administration:

P.o.; 0.5-8 hours
Result:

Produced a reduction of erbB2 tyrosine phosphorylation in FRE-erbB2 xenografts.

Animal Model:

Athymic female mice bearing FRE-erbB2 xenografts^[1]
Dosage:

6.25- 100 mg/kg
Administration:

P.o.; q.d; for 8 to 40 day
Result:

Resulted in an inhibition of FRE-erbB2 xenografts.

Chemical Information

CAS. Nr. 383432-38-0
Appearance Solid
Molecular Weight 469.55
Formel C₂₇H₂₇N₅O₃
Color Light yellow to yellow
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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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Cell Host Microbe

Peptostreptococcus stomatis promotes colonic tumorigenesis and receptor tyrosine kinase inhibitor resistance by activating ERBB2-MAPK. [Abstract]

2024 Jul 23:S1931-3128(24)00254-3. 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

Lösungsmittel & Löslichkeit

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1297 mL

10.6485 mL

21.2970 mL

5 mM

0.4259 mL

2.1297 mL

4.2594 mL

10 mM

0.2130 mL

1.0648 mL

2.1297 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.32 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Jani JP, et al. Discovery and pharmacologic characterization of CP-724,714, a selective ErbB2 tyrosine kinase inhibitor. Cancer Res, 2007, 67(20), 9887-9893. [Content Brief]

[2]. Feng B, et al. Role of hepatic transporters in the disposition and hepatotoxicity of a HER2 tyrosine kinase inhibitor CP-724,714. Toxicol Sci, 2009, 108(2), 492-500. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

CP-724714

4 Cited Publications

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CP-724714

Apoptosis Compound Library

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Publications Citing Use of MedChemExpress (MCE) CP-724714

Alle EGFR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (4)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CP-724714 Related Classifications

HY-14674 Related Classifications