6-(2,6-DICHLORO-PHENYL)-2-(4-FLUORO-3-METHYL-PHENYLAMINO)-8-METHYL-8H-PYRIDO[2,3-D]PYRIMIDIN-7-ONE
6-(2,6-DICHLORO-PHENYL)-2-(4-FLUORO-3-METHYL-PHENYLAMINO)-8-METHYL-8H-PYRIDO[2,3-D]PYRIMIDIN-7-ONE Basic information
- Product Name:
- 6-(2,6-DICHLORO-PHENYL)-2-(4-FLUORO-3-METHYL-PHENYLAMINO)-8-METHYL-8H-PYRIDO[2,3-D]PYRIMIDIN-7-ONE
- 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
- Mol File:
- 287204-45-9.mol
6-(2,6-DICHLORO-PHENYL)-2-(4-FLUORO-3-METHYL-PHENYLAMINO)-8-METHYL-8H-PYRIDO[2,3-D]PYRIMIDIN-7-ONE 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
6-(2,6-DICHLORO-PHENYL)-2-(4-FLUORO-3-METHYL-PHENYLAMINO)-8-METHYL-8H-PYRIDO[2,3-D]PYRIMIDIN-7-ONE 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
6-(2,6-DICHLORO-PHENYL)-2-(4-FLUORO-3-METHYL-PHENYLAMINO)-8-METHYL-8H-PYRIDO[2,3-D]PYRIMIDIN-7-ONESupplier
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