Pictilisib
Cat. No.：YN420271
CAS No. ：957054-30-7
规格
价格(RMB)
库存
| 产品名称: | Pictilisib |
| CAS No.: | 957054-30-7 |
| Chemical Name: | 2-(1H-indazol-4-yl)-6-[[4-(methylsulfonyl)-1-piperazinyl]methyl]-4-(4-morpholinyl)-thieno[3,2-d]pyrimidine |
| Synonyms: | GDC-0941 |
| 分子量: | 513.64 |
| 分子式: | C₂₃H₂₇N₇O₃S₂ |
| SMILES: | CS(N1CCN(CC2=CC3=C(C(N4CCOCC4)=NC(C5=CC=CC6=C5C=NN6)=N3)S2)CC1)(=O)=O |
| 存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
| 运输: | Room temperature in continental US; may vary elsewhere. |
| 产品描述: | Pictilisib (GDC-0941) 是有效的PI3Kα/δ抑制剂，IC50为 3 nM；对110β (11倍) 和 p110γ (25倍) 具有适度的选择性。 |
| IC50和靶点: | [{name:"p110α:3 nM (IC50)"},{name: "p110β:33 nM (IC50)"},{name: "p110δ:3 nM (IC50)"},{name: "p110γ:75 nM (IC50)"},{name: "p110α-H1047R:3 nM (IC50)"},{name: "p110α-E545K:3 nM (IC50)"},{name: "DNA-PK:1.23 μM (IC50)"},{name: "mTOR:0.58 μM (Ki)'}, 'Autophagy'] |
| In Vitro: | |
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| Clinical Trial: | |
| Solvent & Solubility: |
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Folkes, A.J., Ahmadi, K., Alderton, W.K., et al.The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancerJ. Med. Chem.51(18),5522-5532(2008)
Berndt, A., Miller, S., Williams, O., et al.The p110δ structure: Mechanisms for selectivity and potency of new PI(3)K inhibitorsNat. Chem. Biol.6(2),117-124(2010)
Sutherlin, D.P., Sampath, D., Berry, M., et al.Discovery of (thienopyrimidin-2-yl)aminopyrimidines as potent, selective, and orally available pan-PI3-kinase and dual pan-PI3-kinase/mTOR inhibitorsJ. Med. Chem.53(3),1086-1097(2010)
Raynaud, F.I., Eccles, S.A., Patel, S., et al.Biological properties of potent inhibitors of class I phosphatidylinositide 3-kinases: From PI-103 through PI-540, PI-620 to the oral agent GDC-0941Mol. Cancer Ther.8(7),1725-1738(2009)
