PD158780
- CAS No.
- 171179-06-9
- Chemical Name:
- PD158780
- Synonyms
- PD 158780 solution;PD 158780; PD-158780;InSolution? PD 158780;PD158780, 10 mM in DMSO;PD 158780 - CAS 171179-06-9 - Calbiochem;PD 158780, ErbB receptor tyrosine kinase inhibitor;InSolution PD 158780 - CAS 171179-06-9 - Calbiochem;N4-(3-Bromophenyl)-N6-methylpyrido[3,4-d]-4,6-pyrimidinediamine;N4-(3-Bromophenyl)-N6-methyl-pyrido[3,4-d]pyrimidine-4,6-diamine;Pyrido[3,4-d]pyriMidine-4,6-diaMine,N4-(3-broMophenyl)-N6-Methyl-
- CBNumber:
- CB71074528
- Molecular Formula:
- C14H12BrN5
- Molecular Weight:
- 330.18
- MDL Number:
- MFCD00942160
- MOL File:
- 171179-06-9.mol
- MSDS File:
- SDS
- TDS File:
- TDS
| Product description | Number | Pack Size | Price |
| PD 158780 - CAS 171179-06-9 - Calbiochem A potent, cell-permeable, reversible, ATP-competitive inhibitor of the EGFR tyrosine kinase activity (IC?? = 8 pM). | 513035 | 500μg | $189 |
| InSolution PD 158780 - CAS 171179-06-9 - Calbiochem | 513036 | 500μg | $195 |
| PD 158780 >97.0%(HPLC) | P2567 | 10mg | $166 |
| PD 158780 >97.0%(HPLC) | P2567 | 50mg | $582 |
| PD 158780 ≥98% | 13329 | 1mg | $41 |
| Melting point | 174.0 to 178.0 °C |
|---|---|
| Boiling point | 499.6±45.0 °C(Predicted) |
| Density | 1.611±0.06 g/cm3 (20 ºC 760 Torr) |
| storage temp. | Keep in dark place,Inert atmosphere,Store in freezer, under -20°C |
| solubility | DMSO: ≥20mg/mL |
| form | Yellow solid |
| pka | 5.80±0.30(Predicted) |
| color | yellow |
| InChI | 1S/C14H12BrN5/c1-16-13-6-11-12(7-17-13)18-8-19-14(11)20-10-4-2-3-9(15)5-10/h2-8H,1H3,(H,16,17)(H,18,19,20) |
| InChIKey | KFHMLBXBRCITHF-UHFFFAOYSA-N |
| UNSPSC Code | 12352200 |
| NACRES | NA.77 |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Warning | |||||||||
| Hazard statements | H302 | |||||||||
| Precautionary statements | P264-P270-P301+P312-P330-P501 | |||||||||
| Hazard Codes | Xn | |||||||||
| Risk Statements | 22 | |||||||||
| WGK Germany | WGK 2 | |||||||||
| HS Code | 2912.49.2600 | |||||||||
| Storage Class | 10 - Combustible liquids | |||||||||
| NFPA 704 |
|
PD158780 price More Price(63)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Sigma-Aldrich | 513035 | PD 158780 - CAS 171179-06-9 - Calbiochem A potent, cell-permeable, reversible, ATP-competitive inhibitor of the EGFR tyrosine kinase activity (IC?? = 8 pM). | 171179-06-9 | 500μg | $189 | 2025-07-31 | Buy |
| Sigma-Aldrich | 513036 | InSolution PD 158780 - CAS 171179-06-9 - Calbiochem | 171179-06-9 | 500μg | $195 | 2023-01-07 | Buy |
| TCI Chemical | P2567 | PD 158780 >97.0%(HPLC) | 171179-06-9 | 10mg | $166 | 2026-04-30 | Buy |
| TCI Chemical | P2567 | PD 158780 >97.0%(HPLC) | 171179-06-9 | 50mg | $582 | 2026-04-30 | Buy |
| Cayman Chemical | 13329 | PD 158780 ≥98% | 171179-06-9 | 1mg | $41 | 2026-04-30 | Buy |
PD158780 Chemical Properties,Uses,Production
Uses
PD 158780 is a potent tyrosine kinase inhibitor of the epidermal growth factor receptor and has been shown to delay substantial growth of tumors in vivo tumor models.
Definition
ChEBI: PD158780 is a pyridopyrimidine that is pyrido[3,4-d]pyrimidine-4,6-diamine in which the amino groups at positions 4 and 6 are substituted by a m-bromophenyl group and a methyl group, respectively. It is a potent, cell-permeable, reversible ATP-competitive inhibitor of EGFR tyrosine kinase activity [IC50 values of 0.008, 49 and 52 nM for EGFR, ErbB2 (HER2) and Erb4 (HER4)]. It does not inhibit FGF or PDGF-mediated tyrosine phosphorylation. Induces G1 cell cycle arrest in MCF10A cells and is antiproliferative in A431 human epidermal carcinoma cells. It has a role as an antineoplastic agent and an EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor. It is a pyridopyrimidine, a secondary amino compound, a member of bromobenzenes, a diamine and an aromatic amine.
General Description
A potent inhibitor of the EGFR tyrosine kinase activity (8 pM). Also inhibits heregulin-stimulated autophosphorylation in SK-BR-3 (IC50 =49 nM) and MDA-MB-453 (IC50 = 52 nM) breast carcinomas. The inhibition is competitive and results from binding of the inhibitor at the ATP site of the enzymes. Inhibits the LPA-stimulated MAP kinase kinase 1/2 (MKK1/2) activation and EGFR tyrosine phosphorylation in HeLa and NIH3T3 cells.
Biological Activity
Potent inhibitor of ErbB receptor family tyrosine kinases (IC 50 values are 0.008, 49 and 52 nM for EGFR, ErbB2 and ErbB2/ErbB4 respectively) that does not inhibit FGF or PDGF-mediated tyrosine phosphorylation. Induces G 1 cell cycle arrest in MCF10A cells and is antiproliferative in A431 human epidermal carcinoma cells.
Biochem/physiol Actions
Cell permeable: yes
Synthesis
![N-(3-broMophenyl)-6-fluoropyrido[3,4-d]pyriMidin-4-aMine](/CAS/GIF/171179-03-6.gif)
171179-03-6
171179-06-9
Example 60: Synthesis of N4-(3-bromophenyl)-N6-methylpyrido[3,4-d]pyrimidine-4,6-diamine N-(3-Bromophenyl)-6-fluoro-pyrido[3,4-D]pyrimidin-4-amine (0.20 g, 0.63 mmol) was placed in a pressure vessel and an ethanol solution of methylamine was added and reacted at 100 °C. After completion of the reaction, purification was carried out by alumina column chromatography with the eluent dichloromethane/methanol (99:1, v/v) to afford the target product N4-(3-bromophenyl)-N6-methylpyrido[3,4-d]pyrimidine-4,6-diamine (0.07 g, 34% yield). 1H NMR (DMSO) δ 9.69 (1H, s), 8.75 (1H, s), 8.41 (1H, s), 8.21 (1H, brs), 7.93 (1H, brd, J = 7.6 Hz), 7.41-7.28 (2H, m), 7.06 (1H, s), 6.82 (1H, q, J = 5.0 Hz), 4.95 ( 3H, d, J = 5.0 Hz).
storage
Store at -20°C
References
[1] Patent: US5654307, 1997, A
PD158780 Preparation Products And Raw materials
Raw materials
Preparation Products
PD158780 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
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| TargetMol Chemicals Inc. | +1-781-999-5354; | support@targetmol.com | United States | 39037 | 58 |
| ShenZhen Trendseen Biological Technology Co.,Ltd. | 13417589054 | trendseenbio@gmail.com | China | 11680 | 58 |
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| DAYANG CHEM (HANGZHOU) CO.,LTD | +86-88938639 +86-17705817739 | info@dycnchem.com | China | 53803 | 58 |
