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Submit ReviewPD 180970
说明： p210Bcr/Abl kinase inhibitor; also inhibits c-Src and KIT
化学名： 6-(2,6-Dichlorophenyl)-2-[(4-fluoro-3-methylphenyl)amino]-8-methyl-pyrido[2,3-d]pyrimidin-7(8H)-one
纯度： ≥98% (HPLC)
生物活性 for PD 180970
PD 180970 is an ATP-competitive inhibitor of p210bcr/abl tyrosine kinase; selectively induces apoptosis in chronic myeloid leukemia (CML) K562 cells. Inhibits in vivo tyrosine phosphorylation of Gab2, CrkL and p210bcr/abl (IC50 values are 80, 80 and 170 nM respectively). Potently inhibits p210bcr/abl autophosphorylation in vitro (IC50 = 5 nM). Also potently inhibits c-Src and KIT (IC50 values are 0.8 and 50 nM, respectively). Induces autophagy and reduces neuroinflammation in animal models of Parkinson's disease.
许可信息
Sold for research purposes under agreement from Pfizer Inc.
技术数据 for PD 180970
| 分子量 | 429.27 |
| 公式 | C21H15Cl2FN4O |
| 储存 | Store at +4°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 287204-45-9 |
| PubChem ID | 5311104 |
| InChI Key | SLCFEJAMCRLYRG-UHFFFAOYSA-N |
| Smiles | CN(C(C(C4=C(Cl)C=CC=C4Cl)=C3)=O)C1=C3C=NC(NC2=CC(C)=C(F)C=C2)=N1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
产品说明书 for PD 180970
参考文献 for PD 180970
参考文献是支持产品生物活性的出版物。
Dorsey et al (2000) The pyrido[2,3-d]pyrimidine derivative PD180970 inhibits p210bcr-abl tyrosine kinase and induces apoptosis of K562 leukemic cells. Cancer Res. 60 3127 PMID: 10866298
Corbin et al (2004) Sensitivity of oncogenic KIT mutants to the kinase inhibitors MLN518 and PD180970. Blood 104 3754 PMID: 15304388
La Rosée et al (2002) Activity of the Bcr-Abl kinase inhibitor PD180970 against clinically relevant Bcr-Abl isoforms that cause resistance to ima. mesylate (Gleevec, STI571). Cancer Res. 62 7149 PMID: 12499247
Sn et al (2019) Small molecule modulator of aggrephagy regulates neuroinflammation to curb pathogenesis of neurodegeneration. EBioMedicine 50 260 PMID: 31727601
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关键词: PD 180970, PD 180970 supplier, PD180970, Pfizer, Bcr-Abl, tyrosine, kinase, inhibitors, inhibits, c-Src, KIT, Abl, Kinase, Src, Kinases, Other, RTKs, Autophagy, 4965, Tocris Bioscience
1 篇 PD 180970 的引用文献
引用文献是使用了 Tocris 产品的出版物。 PD 180970 的部分引用包括：
Sn et al (2019) Small molecule modulator of aggrephagy regulates neuroinflammation to curb pathogenesis of neurodegeneration. EBioMedicine 50 260 PMID: 31727601
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