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Staurosporine (AM-2282) 是一种蛋白激酶抑制剂,对 PKC、PKA、c-Fgr、Phosphorylase kinase 和 TAOK2 均有抑制活性 (IC50=6/15/2/3/3000 nM),具有 ATP 竞争性和非选择性。Staurosporine 也可以诱导凋亡。
Staurosporine (AM-2282) 是一种蛋白激酶抑制剂,对 PKC、PKA、c-Fgr、Phosphorylase kinase 和 TAOK2 均有抑制活性 (IC50=6/15/2/3/3000 nM),具有 ATP 竞争性和非选择性。Staurosporine 也可以诱导凋亡。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 452 | In stock | |
2 mg | ¥ 659 | In stock | |
5 mg | ¥ 1,190 | In stock | |
10 mg | ¥ 1,880 | In stock | |
25 mg | ¥ 3,660 | In stock | |
50 mg | ¥ 4,990 | In stock | |
100 mg | ¥ 7,160 | In stock | |
500 mg | ¥ 14,300 | In stock | |
1 mL x 10 mM (in DMSO) | ¥ 1,380 | In stock |
Staurosporine 相关产品
产品描述 | Staurosporine (AM-2282) is a protein kinase inhibitor with ATP-competitive and non-selective inhibitory activity (IC50=6/15/2/3/3000 nM) against PKC, PKA, c-Fgr, phosphorylase kinase and TAOK2. Staurosporine also induces apoptosis. |
靶点活性 | PKCη:4 nM, PKCδ:20 nM, PKCζ:1086 nM, PKCε:73 nM, PhK (Phosphorylase kinase):3 nM, CSK:2000 nM, IR:61 nM, IGF-1R:6150 nM, PKCγ:5 nM, EGFR:100 nM, TPK-IIB/Syk:16 nM, MLCK:21 nM, PKCα:2 nM, S6K:5 nM, ERK1:1500 nM, Ca 2+ /CaM PK-I1:20 nM, CK2:19500 nM, PKA:15 nM, v-Src:6 nM, cdc2:9 nM, PhK:3 nM, CK1:163500 nM |
体外活性 | 方法:人宫颈癌细胞 HeLa 用 Staurosporine (1-10 nM) 处理 72 h,使用 MTT 方法检测细胞活力。 |
体内活性 | 方法:为检测体内抗肿瘤活性,将 Staurosporine (3 mg/kg) 和 Lapatinib (50 mg/kg) 灌胃给药给携带人乳腺癌肿瘤 JIMT-1 的 Nu/J-Foxn1 Nu/Nu 小鼠,每周两次,持续两周。 |
激酶实验 | Enzyme assay and binding assay: Protein kinase C is assayed in a reaction mixture (0.25 mL) containing 5 μmol of Tris/HCl, pH 7.5, 2.5 μmol of magnesium acetate, 50 μg of histone II S, 20 μg of phosphatidylserine, 0.88 μg of diolein, 125 nmol of CaCl2, 1.25 nmol of [γ-32]ATP (5-10 × 104 cpm/nmol) and 5 μg of partially purified enzyme. The binding of [3H]PDBu to protein kinase C is determined: Reaction mixture (200 μL contained 4 μmo1 of Tris/malate, pH 6.8, 20 μmol of KCl, 30 nmol of CaC12, 20 μg of phosphatidylserine, 5 μg of partially purified protein kinase C, 0.5% (final concentration) of DMSO,10 pmol of [3H]PDBu (l-3 × 104 cpm/pmol) and 10 μL of various amounts of Staurosporine. |
细胞实验 | Cells are exposed to Staurosporine for ~32 hours. Cells are fixed in 4% paraformaldehyde and stained with the DNA-binding dye Hoechst 33342. Cells are visualized under epifluorescence illumination, and the percentage of apoptotic cells (cells with condensed and fragmented DNA) is determined. (Only for Reference) |
别名 | 星形孢菌素, 星孢菌素, CGP 41251, Antibiotic AM-2282, AM-2282 |
分子量 | 466.53 |
分子式 | C28H26N4O3 |
CAS No. | 62996-74-1 |
Smiles | CN[C@H]1C[C@@H]2O[C@@](C)([C@H]1OC)n1c3ccccc3c3c4CNC(=O)c4c4c5ccccc5n2c4c13 |
密度 | 1.56 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||
溶解度信息 | H2O: < 0.1 mg/mL (insoluble) DMSO: 13.75 mg/mL (29.47 mM), Sonication is recommended. ![]() | |||||||||||||||||||||||||
体内实验配方 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.1 mg/mL (6.64 mM), Solution. 请按顺序添加溶剂,在添加下一种溶剂之前,尽可能使溶液澄清。如有必要,可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考,体内配方并不是绝对的,请根据不同情况进行调整。![]() | |||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||
DMSO
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以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。
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