PD180970 is a novel Bcr-Abl inhbiitor. PD180970 inhibited in vivo tyrosine phosphorylation of p210Bcr-Abl (IC50 = 170 nM) and the p210BcrAbl substrates Gab2 and CrkL (IC50 = 80 nM) in human K562 chronic myelogenous leukemic cells. In vitro, PD180970 potently inhibited autophosphorylation of p210Bcr-Abl (IC50 = 5 nM) and the kinase activity of purified recombinant Abl tyrosine kinase (IC50 = 2.2 nM). Incubation of K562 cells with PD180970 resulted in cell death. PD180970 is among the most potent inhibitors of the p210Bcr-Abl tyrosine kinase, which is present in almost all cases of human chronic myelogenous leukemia. PD180970 is a promising candidate as a novel therapeutic agent for Bcr-Abl-positive leukemia.

CAS 287204-45-9 MFCD10565929

化学结构图

287204-45-9
SMILES: Cc1cc(Nc2ncc3cc(-c4c(Cl)cccc4Cl)c(=O)n(C)c3n2)ccc1F

化学属性

Mol. FormulaC21H15Cl2FN4O
Mol. Weight429.27
Appearance Solid powder
SolubilitySoluble in DMSO

别名和识别编码

Chemical NamePD180970 is a novel Bcr-Abl inhbiitor. PD180970 inhibited in vivo tyrosine phosphorylation of p210Bcr-Abl (IC50 = 170 nM) and the p210BcrAbl substrates Gab2 and CrkL (IC50 = 80 nM) in human K562 chronic myelogenous leukemic cells. In vitro, PD180970 potently inhibited autophosphorylation of p210Bcr-Abl (IC50 = 5 nM) and the kinase activity of purified recombinant Abl tyrosine kinase (IC50 = 2.2 nM). Incubation of K562 cells with PD180970 resulted in cell death. PD180970 is among the most potent inhibitors of the p210Bcr-Abl tyrosine kinase, which is present in almost all cases of human chronic myelogenous leukemia. PD180970 is a promising candidate as a novel therapeutic agent for Bcr-Abl-positive leukemia.
Synonym 6-(2,6-Dichlorophenyl)-2-[(4-fluoro-3-methylphenyl)amino]-8-methyl-pyrido[2,3-d]pyrimidin-7(8H)-one 6-(2,6-Dichlorophenyl)-2-[(4-fluoro-3-methylphenyl)amino]-8-methyl-pyrido[2,3-d]pyrimidin-7(8H)-one PF-1515965 PD180970; PD180970; PD180970; PF1515965. PF-1515965
MDL NumberMFCD10565929
CAS Number287204-45-9
PubChem Substance ID329823727
Chemical Name Translation
FormulaC21H15Cl2FN4O
IUPAC Name6-(2,6-Dichlorophenyl)-2-[(4-fluoro-3-methylphenyl)amino]-8-methyl-pyrido[2,3-d]pyrimidin-7(8H)-one
InChIKeySLCFEJAMCRLYRG-UHFFFAOYSA-N
InChIInChI=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)
Canonical SMILESO=C1C(C2=C(Cl)C=CC=C2Cl)=CC3=CN=C(NC4=CC=C(F)C(C)=C4)N=C3N1C
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分类

  • Approved Therapeutics/Drug Candidates, Cell Biology, Cell Signaling and Neuroscience, Kinase/Phosphatase Biology, Non-Receptor Tyrosine Kinase Biology, Non-Receptor Tyrosine Kinase Inhibitors, Pfizer Compounds, c-Abl
  • {SNA} Approved Therapeutics/Drug Candidates, Bioactive Small Molecule Alphabetical Index, Diversification Ready Pharma-Developed Compounds, Kinase/Phosphatase Biology, Non-Receptor Tyrosine Kinase Biology, Non-Receptor Tyrosine Kinase Inhibitors, P-PH, Pfizer Compounds, c-Abl, 生物活性小分子, 细胞信号转导和神经科学, 细胞生物学

产品应用

  • PD180970 is a novel Bcr-Abl inhbiitor. PD180970 inhibited in vivo tyrosine phosphorylation of p210Bcr-Abl (IC50 = 170 nM) and the p210BcrAbl substrates Gab2 and CrkL (IC50 = 80 nM) in human K562 chronic myelogenous leukemic cells. In vitro, PD180970 potently inhibited autophosphorylation of p210Bcr-Abl (IC50 = 5 nM) and the kinase activity of purified recombinant Abl tyrosine kinase (IC50 = 2.2 nM). Incubation of K562 cells with PD180970 resulted in cell death. PD180970 is among the most potent inhibitors of the p210Bcr-Abl tyrosine kinase, which is present in almost all cases of human chronic myelogenous leukemia. PD180970 is a promising candidate as a novel therapeutic agent for Bcr-Abl-positive leukemia.

相关文献及参考

  • Cowan-Jacob, S.W., et al., Imatinib (STI571) resistance in chronic myelogenous leukemia: molecular basis of the underlying mechanisms and potential strategies for treatment. Mini Rev. Med. Chem. 4 , 285-299, (2004)
  • LaRosee, P., et al., Activity of the Bcr-Abl kinase inhibitor PD180970 against clinically relevant Bcr-Abl isoforms that cause resistance to imatinib mesylate (Gleevec, STI571). Cancer Res. 62 , 7149-7155, (2002)

安全信息

GHS Symbol
Precautionary statements
  • P301+P310
Signal word Danger
Hazard statements
  • H413 Maycauselonglastingharmfuleffectstoaquaticlife 可能对水生生物造成长期持续有害影响。
  • H301 Toxic if swallowed 吞食有毒
WGK Germany3
Safety Statements
  • S45 In case of accident or if you feel unwell seek medical advice immediately (show the label where possible) 发生事故时或感觉不适时，立即求医（可能时出示标签）；
Hazard Codes T
Risk Statements
  • R25 Toxic if swallowed 吞咽有毒
Storage condition Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

系列性分类

  1. Chemical Synthesis 化学合成
  2. Building Blocks 合成砌块
  3. Chemicals by Class 化学分类法
  4. Halogenated 卤化物 (氟氯溴碘)
  5. Fluoro 氟化物
  1. Life Science 生命科学
  2. Cell Biology 细胞生物学
  3. Cell Signaling and Neuroscience - Cell Biology
  4. Kinase/Phosphatase Biology - Cell Signaling and Neuroscience
  5. Non-Receptor Tyrosine Kinase Biology - Kinase/Phosphatase Biology
  6. Non-Receptor Tyrosine Kinase Inhibitors - Non-Receptor Tyrosine Kinase Biology
  7. c-Abl - Non-Receptor Tyrosine Kinase Inhibitors
  1. Medical Research Areas
  2. Angiogenesis
  3. Bcr-Abl
  1. Medical Research Areas
  2. Cytosketetal Signaling
  3. Bcr-Abl

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