PD158780

SKU: orb1301813

Description

PD158780

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 171179-06-9
• MW: 330.18
• Purity: 99.16%
• Formula: C₁₄H₁₂BrN₅
• SMILES: CNc1cc2c(Nc3cccc(Br)c3)ncnc2cn1
• Target: EGFR
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (3.03 mM);Ethanol:8 mg/mL (24.23 mM);DMSO:30 mg/mL (90.86 mM)

Bioactivity

• Target IC50:
  EGFR:0.008 nM (cell free)|EGFR:8 μM (Cell Assay)|ErbB2:49 nM (Cell Assay)|ERB3:52 nM (Cell Assay)|ERB4:52 nM (Cell Assay)
• In Vitro:
  PD158780 inhibited EGF receptor autophosphorylation in A431 human epidermoid carcinoma with IC50 values of 13 nM. PD 158780 was highly specific for the EGF receptor in Swiss 3T3 fibroblasts, inhibiting EGF-dependent receptor autophosphorylation and thymidine incorporation at low nanomolar concentrations. PD 158780 inhibited heregulin-stimulated phosphorylation in the SK-BR-3 and MDA-MB-453 breast carcinomas with IC50 values of 49 and 52 nM, respectively .
• Cell Research:
  All cell lines were maintained as monolayers in dMEM/F12, 50:50 containing 10% fetal bovine serum. For growth inhibition assays, dilutions of the designated compound in 10 μL were placed in 24-well Linbro plates (1.7 x 1.6 cm, flat bottom) followed by the addition of cells (2 × 10^4) in 2 mL of medium. The plates were incubated for 72 hr at 37 °C in a humidified atmosphere containing 5% CO 2 in air. Cell growth was determined by counting cells with a Coulter model AM electronic cell counter. For clone formation in soft agar, cells were trypsinized, and 10,000 cells/mL were seeded into DMEM/F12 medium containing 10% fetal bovine serum, 0.4% agarose, and the designated concentration of compound. One milliliter of this solution was placed over a bottom layer of the same medium containing 0.8% agarose in a 35-mm Petri dish and incubated at 37 °C in a humidified atmosphere containing 5% CO 2 in air. After 3 weeks, colonies were stained with p-iodonitrotetrazolium violet (INT) and quantitated with an image analyzer using the software NIH Image version 1.55. Incorporation of radiolabeled thymidine into cellular DNA was monitored by exposing compound-treated or control cells to [methyl)H]thymidine at a concentration of 1 μM and specific activity of 1 μCi/nmol. After 2 hr the cells were trypsinized and injected into 2 mL of ice-cold 15% trichloroacetic acid (TCA). The resulting precipitate was collected on glass fiber filters, washed five times with 2-mL aliquots of ice-cold 15% TCA, dried, and placed in scintillation vials plus 10 mL Ready gel .

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

HER1, Epidermal growth factor receptor, ErbB-1, ErbB2, EGFR, ErbB4, ErbB3, inhibit, Inhibitor, PD 158780, PD158780, PD-158780

Compound Identifiers

PubChem CID

4707