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EGFR/ErbB2 Inhibitor

Catalog No.GC14856

EGFR/ErbB2 Inhibitor (Compound 5) is a EGFR and ErbB inhibitor with IC50s of 0.017 μM, 0.08 μM, 1.91 μM.

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EGFR/ErbB2 Inhibitor Chemical Structure

Cas No.: 179248-61-4

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5mg
$315.00
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10mg
$522.00
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25mg
$990.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

IC50: 20 and 79 nM for EGFR and c-ErbB2, respectively

EGFR/ErbB2 Inhibitor is an EGFR and c-ErbB2 inhibitor.

EGFR and c-ErbB-2 are members of the epidermal growth factor receptor subfamily of protein tyrosine kinases. Their cellular overexpression causes transformation, so that the cells will grow in the absence of growth factors. An inhibitor of thse kinases should block the receptor signalling, subsequent transformation and inappropriate growth.

In vitro: EGFR/ErbB2 Inhibitor was identified as a potent inhibitor of both c-erbB-2 and EGFr [IC50: 0.079 μM for c-erbB-2, 0.020 μM for EGFr (isolated enzyme), 2.0 μM for HB4aC5.2 cells, 1.2 μM for BT474, both overexpressing c-erbB-2; 2.5 μM for HN5 cells overexpressing EGFr]. This combined potency was contrast to smaller, previously reported anilinoquinazolines and its subsequent analogues [1].

In vivo: GW974, a analog of EGFR/ErbB2 Inhibitor, was evaluated in the fast growing N87 gastric tumour xenograft in SCID mice. Results showed that GW974 at bid dose of 10 mg/kg po led to a 50% inhibition of tumour growth over the 20-day dosing period. Moreover, GW974 at 10 mg/kg po bid had complete inhibition of tumour growth over the 20-day dosing period in the BT474 breast tumour xenograft model. A longer-term study with initial dosing at 30 mg/kg po bid produced tumour shrinkage [1].

Clinical trial: Up to now, EGFR/ErbB2 Inhibitor is still in the preclinical development stage.

Reference:
[1] S.  Cockerill, C. Stubberfield, J. Stables, et al. Indazolylamino quinazolines and pyridopyrimidines as inhibitors of the EGFr and C-erbB-2. Bioorganic & Medicinal Chemistry Letters 11, 1401-1405 (2001).

Chemical Properties

Cas No. 179248-61-4 SDF
Chemical Name 6,7-dimethoxy-N-[4-(phenylmethoxy)phenyl]-4-quinazolinamine
Canonical SMILES COC1=C(OC)C=C(C(NC2=CC=C(OCC3=CC=CC=C3)C=C2)=NC=N4)C4=C1
Formula C23H21N3O3 M.Wt 387.4
Solubility ≤1mg/ml in DMSO;10mg/ml in dimethyl formamide Storage 4°C, protect from light
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.5813 mL 12.9066 mL 25.8131 mL
5 mM 0.5163 mL 2.5813 mL 5.1626 mL
10 mM 0.2581 mL 1.2907 mL 2.5813 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 33 reference(s) in Google Scholar.)

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