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Submit ReviewPF 05212384
说明： Potent and selective dual PI 3-K/mTOR inhibitor
别名： PKI-587,Gedatolisib
化学名： N-[4-[[4-(Dimethylamino)-1-piperidinyl]carbonyl]phenyl]-N'-[4-(4,6-di-4-morpholinyl-1,3,5-triazin-2-yl)phenyl]urea
纯度： ≥98% (HPLC)
生物活性 for PF 05212384
PF 05212384 is a potent and selective dual inhibitor of PI 3-kinase/mTOR (IC50 values are 0.4, 1.6 and 5.4 nM for PI 3-Kα, mTOR and PI 3-Kγ respectively). Exhibits selectivity over 234 other protein kinases (IC50 >10 μM). Potently inhibits tumor cell growth in 37 different tumor cell lines (IC50 < 100 nM). Also exhibits antitumor activity in MDA-361, HCT-116, H1975 and U87MG xenograft models.
许可信息
Sold for research purposes under agreement from Pfizer Inc.
技术数据 for PF 05212384
| 分子量 | 615.73 |
| 公式 | C32H41N9O4 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 1197160-78-3 |
| PubChem ID | 44516953 |
| InChI Key | DWZAEMINVBZMHQ-UHFFFAOYSA-N |
| Smiles | O=C(NC5=CC=C(C(N6CCC(N(C)C)CC6)=O)C=C5)NC(C=C4)=CC=C4C1=NC(N2CCOCC2)=NC(N3CCOCC3)=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 PF 05212384
参考文献 for PF 05212384
参考文献是支持产品生物活性的出版物。
Venkatesan et al (2010) Bis(morpholino-1,3,5-triazine) derivatives: potent adenosine 5'-triphosphate competitive phosphatidylinositol-3-kinase/mammalian target of rapamycin inhibitors: discovery of compound 26 (PKI-587), a highly efficacious dual inhibitor. J.Med.Chem. 53 2636 PMID: 20166697
Mallon et al (2011) Antitumor efficacy of PKI-587, a highly potent dual PI3K/mTOR kinase inhibitor. Clin.Cancer Res. 17 3193 PMID: 21325073
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关键词: PF 05212384, PF 05212384 supplier, PF05212384, antitumor, antitumour, PI3-K, phosphoinositide, 3-kinases, mTOR, mammalian, target, of, rapamycin, inhibitors, inhibits, PKI587, Pfizer, PKI-587, Gedatolisib, PI, 3-Kinase, 4823, Tocris Bioscience
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