| Identification | Back Directory | [Name]
PD180970 | [CAS]
287204-45-9 | [Synonyms]
PD 180790
PD 180970
PF-1515965
PD-180970,PD180970
6-(2,6-dichlorophenyl)-2-(4-fluoro-3-methylanilino)-8-methylpyrido[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
6-(2,6-Dichlorophenyl)-2-[(4-fluoro-3-methylphenyl)amino]-8-methyl-pyrido[2,3-d]pyrimidin-7(8H)-one
PYRIDO[2,3-D]PYRIMIDIN-7(8H)-ONE, 6-(2,6-DICHLOROPHENYL)-2-[(4-FLUORO-3-METHYLPHENYL)AMINO]-8-METHYL- | [Molecular Formula]
C21H15Cl2FN4O | [MDL Number]
MFCD10565929 | [MOL File]
287204-45-9.mol | [Molecular Weight]
429.27 |
| Chemical Properties | Back Directory | [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 | [form ]
A solid | [pka]
3.02±0.20(Predicted) | [color ]
yellow |
| Hazard Information | Back Directory | [Uses]
PD 180970 is an ATP-competitive inhibitor of p210 tyrosine kinase which selectively induces apoptosis in chronic myeloid leukemia (CML) K562 cells. | [Biological Activity]
PD-180970 is a potent inhibitor of the p210 Bcr-Abl tyrosine kinase. | [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 |
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| Company Name: |
Energy Chemical
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| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
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