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PD 158780

Catalog No.GC15925

PD 158780 est un puissant inhibiteur de la famille EGFR avec des IC50 de 8 pM, 49, 52, 52 nM pour EGFR, ErbB2, ErbB3 et ErbB4, respectivement.

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PD 158780 Chemical Structure

Cas No.: 171179-06-9

Taille Prix Stock Qté
5mg
57,00 $US
En stock
10mg
100,00 $US
En stock
25mg
214,00 $US
En stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Kinase experiment:

The enzyme assay is performed in 96-well filter plates. The total volume is 0.1 mL containing 20 mM HEPES, pH 7.4, 50 μM sodium vanadate, 40 mM magnesium chloride, 10 μM ATP containing 0.5 μCi of [32p]ATP, 20 μg of polyglutamic acid/tyrosine, 1 ng of EGF receptor tyrosine kinase, ard appropriate dilutions of inhibitor (PD158780) and/or ATP. All corrtponents except the ATP are added to the well, and the plate is incubated with shaking for 10 min at 25°C. The reaction is started by adding [32p]ATP, and the plate is incubated with shaking at 25°C for 10 min. The reaction is terminated by the addition of 0.1 mL of 20% TCA, and the plate is kept at 4°C for at least 15 min to allow the substrate to precipitate. The wells are then ished five times with 0.125 mL of 10% TCA, and [32p] incorporation is determined[1].

Cell experiment:

All cell lines are maintained as monolayers in dMEM/F12, 50:50 containing 10% fetal bovine serum. For growth inhibition assays, dilutions of the designated compound (PD158780) in 10 μL are placed in 24-well plates followed by the addition of cells in 2 mL of medium. The plates are incubated for 72 hr at 37°C in a humidified atmosphere. Cell growth is determined by counting cells[1].

Animal experiment:

Tumor fragments were implanted sc into the right axilla of mice on day 0. PD158780 is administered intraperitoneally or orally. Tumor growth is monitored[1].

References:

[1]. Fry DW, et al. Biochemical and antiproliferative properties of 4-[ar(alk)ylamino]pyridopyrimidines, a new chemical class of potent and specific epidermal growth factor receptor tyrosine kinase inhibitor. Biochem Pharmacol. 1997 Oct 15;54(8):877-87.

Background

PD158780 is a potent EGFR family inhibitor with IC50s of 8 pM, 49, 52, 52 nM for EGFR, ErbB2, ErbB3, and ErbB4, respectively.

PD158780 inhibits EGF receptor autophosphorylation in A431 human epidermoid carcinoma with IC50 value of 13 nM. PD158780 is highly specific for the EGF receptor in Swiss 3T3 fibroblasts, inhibiting EGF-dependent receptor autophosphorylation and thymidine incorporation at low nanomolar concentrations while requiring micromolar levels for platelet-derived growth factor- and basic fibroblast growth factordependent processes. PD158780 inhibits heregulin-stimulated phosphorylation in the SK-BR-3 and MDAMB-453 breast carcinomas with IC50 values of 49 and 52 nM, respectively, suggesting that the compound is active against other members of the EGF receptor family[1].

PD158780 is active against clone formation in several breast tumors having different expression patterns of the ErbB family. PD158780 shows good therapeutic effect against the A431 epidermoid carcinoma when administered either intraperitoneally or orally. PD158780 produces measurable, significant effects against a mouse fibroblast transfected with human EGFR. PD158780 produces a significant therapeutic effect against the estrogendependent MCF-7 breast carcinoma at equitoxic dose levels[1].

References:
[1]. Fry DW, et al. Biochemical and antiproliferative properties of 4-[ar(alk)ylamino]pyridopyrimidines, a new chemical class of potent and specific epidermal growth factor receptor tyrosine kinase inhibitor. Biochem Pharmacol. 1997 Oct 15;54(8):877-87.

Chemical Properties

Cas No. 171179-06-9 SDF
Chemical Name N4-(3-bromophenyl)-N6-methylpyrido[3,4-d]pyrimidine-4,6-diamine
Canonical SMILES BrC1=CC(NC2=NC=NC3=C2C=C(NC)N=C3)=CC=C1
Formula C14H12BrN5 M.Wt 330.18
Solubility DMF: 30 mg/ml,DMSO: 10 mg/ml,Ethanol: 2 mg/ml Storage Store at -20°C
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 3.0287 mL 15.1433 mL 30.2865 mL
5 mM 0.6057 mL 3.0287 mL 6.0573 mL
10 mM 0.3029 mL 1.5143 mL 3.0287 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 12 reference(s) in Google Scholar.)

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