Bortezomib 硼替佐米;保特佐米
Bortezomib是有效的蛋白酶抑制剂,Ki为0.6 nM。它对肿瘤细胞表现出良好的选择性。Bortezomib可抑制 NF-κB 并诱导 ERK 的磷酸化从而抑制cathepsin B并在卵巢癌和其他固体肿瘤中抑制自噬的催化过程。
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货号:
TK0153 -
规格:
- 1mg
- 5mg
- 10mg
- 50mg
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价格:
¥0.00
Bortezomib是有效的蛋白酶抑制剂,Ki为0.6 nM。它对肿瘤细胞表现出良好的选择性。Bortezomib可抑制 NF-κB 并诱导 ERK 的磷酸化从而抑制cathepsin B并在卵巢癌和其他固体肿瘤中抑制自噬的催化过程。
| CAS No. | 179324-69-7 |
| 生物活性 | Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Anti-cancer activity. |
| 分子式 | C19H25BN4O4 |
| 分子量 | 384.24 |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存条件 | Powder, -20°C ,3 years |
| 溶解性数据 | DMSO : 100 mg/mL (260.25 mM; Need ultrasonic),Ethanol : 66.67 mg/mL (173.51 mM; ultrasonic and warming and heat to 60°C) |
| 体内研究 | Bortezomib (PS-341) (0.3-1 mg/kg; i.v.; once weekly for 4 weeks) inhibits PC-3 Tumor Growth in Nude Mice. |
| 体外研究 | Bortezomib (PS-341) (100 nM; 8 hours) results in the accumulation of cells in G2-M, with a corresponding decrease in the number of cells in G1.Bortezomib (PS-341) (5-100 nM; 20 hours) induces apoptosis in mantle-cell lymphoma (MCL) cell lines.Bortezomib (PS-341) (20 nM; 1-14 hours) induces Noxa up-regulation in both MCL cell lines.The IC50 of Bortezomib (PS-341) is found to be 2.46 nM for 26S proteasome in the B16F10 cells.Bortezomib (PS-341) suppresses several anti-apoptotic proteins (e.g., Bcl-XL, Bcl-2, and STAT-3). |
| 纯度及产品资料 | 98% |