| 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 | [InChI]
1S/C21H15Cl2FN4O/c1-11-8-13(6-7-17(11)24)26-21-25-10-12-9-14(20(29)28(2)19(12)27-21)18-15(22)4-3-5-16(18)23/h3-10H,1-2H3,(H,25,26,27) | [InChIKey]
SLCFEJAMCRLYRG-UHFFFAOYSA-N | [SMILES]
CN1C(=O)C(=Cc2cnc(Nc3ccc(F)c(C)c3)nc12)c4c(Cl)cccc4Cl |
| Safety Data | Back Directory | [Hazard Codes ]
T | [Risk Statements ]
25 | [Safety Statements ]
45 | [RIDADR ]
UN 2811 6.1 / PGIII | [WGK Germany ]
3 | [Storage Class]
6.1C - Combustible acute toxic Cat.3
toxic compounds or compounds which causing chronic effects | [Hazard Classifications]
Acute Tox. 3 Oral
Aquatic Chronic 4 |
| 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 | [in vivo]
PD180970 (5 mg/kg; intraperitonial injection; daily; for 7 days) mitigates MPTP-induced neuronal loss in mice. PD180970 has the neuroprotective ability in a preclinical mouse model of Parkinson's disease (PD)[4]. | Animal Model: | Male C57BL/6J mice (3-4 months old) injected with MPTP[4] | | Dosage: |
5?mg/kg
| | Administration: | Intraperitonial injection; daily; for 7 days | | Result: | Decreased number of activated microglia on activation by MPTP in mice brains. And showed significant reduction in intensity of Iba1 expression in activated microglia. |
| [IC 50]
Bcr-Abl: 5 nM (IC50, p210Bcr-Abl kinase); Src: 0.8 nM (IC50); KIT: 50 nM (IC50) |
|
| Company Name: |
Energy Chemical
|
| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
|