注：本產品僅用于科研，不可用于臨床
Bortezomib抑制劑 生物活性
tezomib (ps - 341)是一個可逆的和有選擇性的蛋白酶體抑制劑,20年代,強有力地抑制蛋白酶體(Ki = 0.6海里)通過瞄準一個threonine殘基。Bortezomib干擾細胞周期、凋亡和抑制NF-κB。Bortezomib是Di一蛋白酶體抑制劑抗癌劑
Bortezomib抑制劑 IC50 & Target
Ki: 0.6 nM (20S proteasome)[1]
體外研究
(In Vitro) | 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[1].
Bortezomib (PS-341) (5-100 nM; 20 hours) induces apoptosis in mantle-cell lymphoma (MCL) cell lines[3].
Bortezomib (PS-341) (20 nM; 1-14 hours) induces Noxa up-regulation in both MCL cell lines[3].
The IC50 of Bortezomib (PS-341) is found to be 2.46 nM for 26S proteasome in the B16F10 cells[4].
Bortezomib (PS-341) suppresses several anti-apoptotic proteins (e.g., Bcl-XL, Bcl-2, and STAT-3)[5]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Cycle Analysis[1] | Cell Line: | PC-3 cells | | Concentration: | 100 nM | | Incubation Time: | 8 hours | | Result: | Resulted in the accumulation of cells in G2-M, with a corresponding decrease in the number of cells in G1. |
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體內研究
(In Vivo) | Bortezomib (PS-341) (0.3-1 mg/kg; i.v.; once weekly for 4 weeks) inhibits PC-3 Tumor Growth in Nude Mice[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only. | Animal Model: | Male nude mice (xenograft tumor model bearing PC-3 cells)[1] | | Dosage: | 0.3, 1 mg/kg | | Administration: | Intravenous injection; once weekly for 4 weeks | | Result: | Resulted in a significant decrease in tumor growth ~60% at dose of 1 mg/kg. |
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| 運輸條件 | Room temperature in continental US; may vary elsewhere. |
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| 溶解性數(shù)據(jù) | In Vitro: Ethanol : 66.67 mg/mL (173.51 mM; ultrasonic and warming and heat to 60°C) DMSO : 50 mg/mL (130.13 mM; Need ultrasonic) 配制儲備液 | 1 mM | 2.6025 mL | 13.0127 mL | 26.0254 mL | | 5 mM | 0.5205 mL | 2.6025 mL | 5.2051 mL | | 10 mM | 0.2603 mL | 1.3013 mL | 2.6025 mL |
*請根據(jù)產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 儲存時，請在 6 個月內使用，-20°C 儲存時，請在 1 個月內使用。 In Vivo: 請根據(jù)您的實驗動物和給藥方式選擇適當?shù)娜芙夥桨?。以下溶解方案都請先按?In Vitro 方式配制澄清的儲備液，再依次添加助溶劑： ——為保證實驗結果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當保存；體內實驗的工作液，建議您現(xiàn)用現(xiàn)配，當天使用； 以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶 1.
請依序添加每種溶劑： 10% EtOH 40% PEG300 5% Tween-80 45% saline Solubility: ≥ 4 mg/mL (10.41 mM); Clear solution
2.
請依序添加每種溶劑： 10% EtOH 90% (20% SBE-β-CD in saline) Solubility: ≥ 4 mg/mL (10.41 mM); Clear solution
3.
請依序添加每種溶劑： 10% EtOH 90% corn oil Solubility: ≥ 4 mg/mL (10.41 mM); Clear solution
4.
請依序添加每種溶劑： 5% DMSO 40% PEG300 5% Tween-80 50% saline Solubility: ≥ 2.5 mg/mL (6.51 mM); Clear solution
5.
請依序添加每種溶劑： 5% DMSO 95% (20% SBE-β-CD in saline) Solubility: ≥ 2.5 mg/mL (6.51 mM); Clear solution
6.
請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (5.41 mM); Clear solution
7.
請依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in saline) Solubility: ≥ 2.08 mg/mL (5.41 mM); Clear solution
8.
請依序添加每種溶劑： 10% DMSO 90% corn oil Solubility: ≥ 2.08 mg/mL (5.41 mM); Clear solution
9.
請依序添加每種溶劑： 1% DMSO 99% saline Solubility: ≥ 0.5 mg/mL (1.30 mM); Clear solution
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