1. Protein Tyrosine Kinase/RTK
    JAK/STAT Signaling
  2. EGFR
  3. PD158780

PD158780 

Cat. No.: HY-18609 Purity: 98.04%
Handling Instructions

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

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

PD158780 Chemical Structure

PD158780 Chemical Structure

CAS No. : 171179-06-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 178 In-stock
Estimated Time of Arrival: December 31
10 mg USD 162 In-stock
Estimated Time of Arrival: December 31
50 mg USD 706 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Description

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

IC50 & Target[1]

EGFR

8 μM (IC50, Cell Assay)

ErbB2

49 nM (IC50, Cell Assay)

ErbB3

52 nM (IC50, Cell Assay)

ErbB4

52 nM (IC50, Cell Assay)

In Vitro

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].

In Vivo

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].

Molecular Weight

330.18

Formula

C₁₄H₁₂BrN₅

CAS No.

171179-06-9

SMILES

CNC1=CC2=C(NC3=CC(Br)=CC=C3)N=CN=C2C=N1

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 : 21 mg/mL (63.60 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[1]

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].

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

Cell Assay
[1]

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].

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

Animal Administration
[1]

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].

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

References
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Keywords:

PD158780PD 158780PD-158780EGFREpidermal growth factor receptorErbB-1HER1Inhibitorinhibitorinhibit

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