|
|
| | PD180970 Basic information |
| Product Name: | PD180970 | | Synonyms: | 6-(2,6-DICHLORO-PHENYL)-2-(4-FLUORO-3-METHYL-PHENYLAMINO)-8-METHYL-8H-PYRIDO[2,3-D]PYRIMIDIN-7-ONE;PD 180790;PD 180970;PYRIDO[2,3-D]PYRIMIDIN-7(8H)-ONE, 6-(2,6-DICHLOROPHENYL)-2-[(4-FLUORO-3-METHYLPHENYL)AMINO]-8-METHYL-;6-(2,6-Dichlorophenyl)-2-[(4-fluoro-3-methylphenyl)amino]-8-methyl-pyrido[2,3-d]pyrimidin-7(8H)-one;PF-1515965;6-(2,6-dichlorophenyl)-2-(4-fluoro-3-methylanilino)-8-methylpyrido[2,3-d]pyrimidin-7-one;PD-180970,PD180970 | | CAS: | 287204-45-9 | | MF: | C21H15Cl2FN4O | | MW: | 429.27 | | EINECS: | | | Product Categories: | | | Mol File: | 287204-45-9.mol |  |
| | PD180970 Chemical Properties |
| Boiling point | 590.6±60.0 °C(Predicted) | | density | 1.449±0.06 g/cm3(Predicted) | | storage temp. | 2-8°C | | solubility | DMSO: >20mg/mL | | pka | 3.02±0.20(Predicted) | | form | A solid | | color | yellow |
| Hazard Codes | T | | Risk Statements | 25 | | Safety Statements | 45 | | RIDADR | UN 2811 6.1 / PGIII | | WGK Germany | 3 |
| | PD180970 Usage And Synthesis |
| Uses | PD 180970 is an ATP-competitive inhibitor of p210 tyrosine kinase which selectively induces apoptosis in chronic myeloid leukemia (CML) K562 cells. | | Enzyme inhibitor | This pyridopyrimidine (FWfree-base = 429.28 g/mol) inhibits Bcr-Abl proteintyrosine kinase and induces apoptosis of K562 leukemic cells. In vitro, PD180970 potently inhibited p210Bcr-Abl autophosphorylation (IC50 = 5 nM) as well as the kinase activity of purified Abl tyrosine kinase (IC50 = 2.2 nM). Incubation of K562 cells with PD180970 resulted in cell death, with results of nuclear staining, apoptotic-specific poly(ADP-ribose) polymerase cleavage, and annexin V binding assays confirming as much. Significantly, PD180970 is without effect on the growth and viability of p210Bcr-Ablnegative HL60 human leukemic cells. Such findings demonstrate that PD180970 is among the most potent known inhibitors of the p210Bcr-Abl tyrosine kinase and that it is a promising candidate as a novel therapeutic agent for Bcr-Abl-positive leukemia |
| | PD180970 Preparation Products And Raw materials |
|