|
ChemicalBook Optimization Suppliers |
|
| 化学名: | BI-2536 | | 英語化学名: | BI 2536 | | 别名: | BI-2536, BoehringerPLK-1 inhibitor;4-[[(7R)-8-Cyclopentyl-7-ethyl-5,6,7,8-tetrahydro-5-methyl-6-oxo-2-pteridinyl]amino]-3-methoxy-N-(1-methyl-4-piperidinyl)benzamide;BI 2536;Benzamide, 4-[[(7R)-8-cyclopentyl-7-ethyl-5,6,7,8-tetrahydro-5-methyl-6-oxo-2-pteridinyl]amino]-3-methoxy-N-(1-methyl-4-piperidinyl)-;Boehringer PLK-1 inhibitor;BI-2536(R-);BI2536/BI-2536;(R)-4-((8-cyclopentyl-7-ethyl-5-Methyl-6-oxo-5,6,7,8-tetrahydropteridin-2-yl)aMino)-3-Methoxy-N-(1-Methylpiperidin-4-yl)benzaMide | | CAS番号: | 755038-02-9 | | 分子式: | C28H39N7O3 | | 分子量: | 521.65 | | EINECS: | 1308068-626-2 | | カテゴリ情報: | Inhibitors;API | | Mol File: | 755038-02-9.mol |  |
| 比重(密度) | 1.28 | | 貯蔵温度 | Keep in dark place,Sealed in dry,Store in freezer, under -20°C | | 溶解性 | Soluble in DMSO (up to 20 mg/ml) or in Ethanol (up to 25 mg/ml) | | 外見 | Yellow powder. | | 酸解離定数(Pka) | 14.09±0.20(Predicted) | | 色 | Off-white | | 安定性： | Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months. |
| | BI-2536 Usage And Synthesis |
| 説明 | BI 2536 (755038-02-9) was originally reported as a potent (IC50’s Plk1 = 0.83nM, Plk2 = 3.5nM and Plk3 = 9.0nM)1?and selective2?Polo-like kinase inhibitor?that caused mitotic arrest and apoptosis induction in various human cancer cell lines.1?It was later found to be a potent inhibitor (IC50?= 100nM) of BET family member BRD4 and able to potently suppress c-Myc expression in MM.1S multiple myeloma cells.3?BI 2536 destabilizes N-Myc by inhibiting the deactivation of the ubiquitin E3 ligase Fbw7 by Plk1.4 | | 使用 | BI 2536 is a PLK1 inhibitor, inducing apoptosis together with micro-tubule-destabilizing drugs in preclinical rhabdomyosarcoma models. Anti-cancer and potent PLK1 inhibitor. | | target | Plk1 | | 参考文献 | 1) Steegmaier?et al.?(2007),?BI 2536, a Potent and Selective Inhibitor of Polo-like Kinase 1, Inhibits Tumor Growth In Vivo; Curr. Biol.,?17?316
2) Davis?et al.?(2011),?Comprehensive analysis of kinase inhibitor selectivity; Nat. Biotechnol.,?29?1046
3) Ciceri?et al.?(2014),?Dual kinase-bromodomain inhibitors for rationally designed polypharmacology; Nat. Chem. Biol.,?10?305
4) Xiao?et al.?(2016),?Polo-like Kinase-1 Regulates Myc Stabilization and Activates a Feedforward Circuit Promoting Tumor Cell Survival; Mol. Cell,?64?493 |
|