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

CP-724714 

Cat. No.: HY-14674 Purity: 99.62%
Handling Instructions

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
10 mM * 1 mL in DMSO USD 119 In-stock
Estimated Time of Arrival: December 31
5 mg USD 108 In-stock
Estimated Time of Arrival: December 31
10 mg USD 194 In-stock
Estimated Time of Arrival: December 31
50 mg USD 576 In-stock
Estimated Time of Arrival: December 31
100 mg USD 858 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of CP-724714:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

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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)

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].

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].

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

469.53

Formula

C₂₇H₂₇N₅O₃

CAS No.

383432-38-0

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.[(E)]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (106.49 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1298 mL 10.6489 mL 21.2979 mL
5 mM 0.4260 mL 2.1298 mL 4.2596 mL
10 mM 0.2130 mL 1.0649 mL 2.1298 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References

Purity: 99.62%

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Keywords:

CP-724714CP724714CP 724714EGFRApoptosisEpidermal growth factor receptorErbB-1HER1autophosphorylationselectiveoralcellcycleathymicmiceInhibitorinhibitorinhibit

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Product Name:
CP-724714
Cat. No.:
HY-14674
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