Umbralisib
Cat. No.：YN420114
CAS No. ：1532533-67-7
规格
价格(RMB)
库存
| 产品名称: | Umbralisib |
| CAS No.: | 1532533-67-7 |
| Chemical Name: | 2-[(1S)-1-[4-amino-3-[3-fluoro-4-(1-methylethoxy)phenyl]-1H-pyrazolo[3,4-d]pyrimidin-1-yl]ethyl]-6-fluoro-3-(3-fluorophenyl)-4H-1-benzopyran-4-one |
| Synonyms: | TGR-1202; RP5264 |
| 分子量: | 571.55 |
| 分子式: | C₃₁H₂₄F₃N₅O₃ |
| SMILES: | O=C1C(C2=CC=CC(F)=C2)=C([C@@H](N3N=C(C4=CC=C(OC(C)C)C(F)=C4)C5=C(N)N=CN=C53)C)OC6=CC=C(F)C=C16 |
| 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: | Umbralisib (TGR-1202) 是PI3Kδ抑制剂，IC50和EC50值分别为 22.2 nM 和 24.3 nM；Umbralisib (TGR-1202) 同时可抑制CK1ε，EC50值为 6.0 μM。 |
| IC50和靶点: | [{name:"PI3Kδ:22.2 nM (EC50)"},{name: "PI3Kδ:6.2 nM (Kd)"},{name: "PI3Kγ:1400 nM (Kd)"},{name: "PI3Kβ:>10000 nM (Kd)"},{name: "PI3Kα:>10000 nM (Kd)"}] |
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| Solvent & Solubility: |
Lampson, B.L., and Brown, J.R.PI3Kδ-selective and PI3Kα/δ-combinatorial inhibitors in clinical development for B-cell non-Hodgkin lymphomaExpert Opin. Investig. Drugs26(11),1267-1279(2017)
Deng, C., Lipstein, M.R., Scotto, L., et al.Silencing c-Myc translation as a therapeutic strategy through targeting PI3Kδ and CK1ε in hematological malignanciesBlood129(1),88-99(2017)
Friedman, D.R., Lanasa, M.C., Brander, D.M., et al.Comparison of the PI3K-δ inhibitors TGR1202 and GS-1101 in inducing cytotoxicity and inhibiting phosphorylation of Akt in CLL cells in vitroBlood120(21),3914(2012)
