2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Apoptosis
  3. EGFR Apoptosis
  4. CP-724714

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.

For research use only. We do not sell to patients.

CP-724714 Chemical Structure

CP-724714 Chemical Structure

CAS No. : 383432-38-0

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 119 In-stock
Solution
10 mM * 1 mL in DMSO USD 119 In-stock
Solid
5 mg USD 108 In-stock
10 mg USD 194 In-stock
50 mg USD 576 In-stock
100 mg USD 858 In-stock
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Customer Review

Based on 4 publication(s) in Google Scholar

Other Forms of CP-724714:

CP-724714 Related Antibodies

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EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1][2].

IC50 & Target[1]

ErbB2

10 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
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]
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.

CP-724714 Related Antibodies

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.
Molecular Weight

469.55

Formula

C27H27N5O3
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1297 mL 10.6485 mL 21.2970 mL
5 mM 0.4259 mL 2.1297 mL 4.2594 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.

  • 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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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.

    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:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 98.53%

SDS (251 KB)

COA (245 KB) LCMS (267 KB)

Handling Instructions (2659 KB)
References

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
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CP-724714 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CP-724714383432-38-0CP724714CP 724714EGFRApoptosisEpidermal growth factor receptorErbB-1HER1autophosphorylationselectiveoralcellcycleathymicmiceInhibitorinhibitorinhibit

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