Bortezomib (硼替佐米）

Bortezomib (PS-341) 是一種可逆性和選擇性的蛋白酶體 (proteasome) 抑制劑，通過靶向蘇氨酸殘基有效抑制 20S 蛋白酶體 (Ki=0.6 nM)。Bortezomib 破壞細胞周期、誘導細胞凋亡以及抑制核因子 NF-κB。Bortezomib 是第一種蛋白酶體抑制劑，具有抗ai活性。

貨號：HY-10227
CAS：179324-69-7

參數品牌：MCE

產品參數

品牌：MCE

型號：HY-10227

起訂量：1

規(guī)格:：5 mg

價格:：￥510

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產品詳情

Bortezomib (Synonyms: 硼替佐米）

Bortezomib (PS-341) 是一種可逆性和選擇性的蛋白酶體 (proteasome) 抑制劑，通過靶向蘇氨酸殘基有效抑制 20S 蛋白酶體 (K_i=0.6 nM)。Bortezomib 破壞細胞周期、誘導細胞凋亡以及抑制核因子 NF-κB。Bortezomib 是第一種蛋白酶體抑制劑，具有抗ai活性。

生物活性

Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (K_i=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^[1]^[2].

IC₅₀ & Target：Ki: 0.6 nM (20S proteasome)

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.

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.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT03117751	St. Jude Children′s Research Hospital\|Incyte Corporation\|Amgen\|Servier	Acute Lymphoblastic Leukemia\|Acute Lymphoblastic Lymphoma	March 29, 2017	Phase 2\|Phase 3
NCT04268199	AHS Cancer Control Alberta\|Tom Baker Cancer Centre	Myeloma\|Myeloma Multiple	May 29, 2020	Phase 2
NCT00006362	Mayo Clinic\|National Cancer Institute (NCI)	Leukemia\|Lymphoma\|Multiple Myeloma and Plasma Cell Neoplasm\|Precancerous Condition\|Unspecified Adult Solid Tumor, Protocol Specific	November 1999	Phase 1

分子量：384.24

Formula：C₁₉H₂₅BN₄O₄

CAS 號：179324-69-7

中文名稱：硼替佐米；保特佐米

運輸條件：Room temperature in continental US; may vary elsewhere.

儲存方式：

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性數據

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

濃度溶劑體積質量	1 mg	5 mg	10 mg

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:

以下溶解方案都請先按照 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儲存條件，適當保存；體內實驗的工作液，建議您現用現配，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沉淀、析出現象，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

參考文獻

[1]. Adams J, et al. Proteasome inhibitors: a novel class of potent and effective antitumor agents. Cancer Res. 1999 Jun 1;59(11):2615-22.

[2]. Shahshahan MA, et al. Potential usage of proteasome inhibitor bortezomib (Velcade, PS-341) in the treatment of metastaticmelanoma: basic and clinical aspects. Am J Cancer Res. 2011;1(7):913-24.

[3]. Pérez-Galán P, et al. The proteasome inhibitor bortezomib induces apoptosis in mantle-cell lymphoma through generation of ROS and Noxa activation independent of p53 status. Blood. 2006 Jan 1;107(1):257-64.

[4]. Yerlikaya A, et al. Combined effects of the proteasome inhibitor bortezomib and Hsp70 inhibitors on the B16F10 melanoma cell line. Mol Med Rep. 2010 Mar-Apr;3(2):333-9.

[5]. Mujtaba T, et al. Advances in the understanding of mechanisms and therapeutic use of bortezomib. Discov Med. 2011 Dec;12(67):471-80.

[6]. Fernández Y, et al. Chemical blockage of the proteasome inhibitory function of bortezomib: impact on tumor cell death. J Biol Chem. 2006 Jan 13;281(2):1107-18.

Bortezomib (硼替佐米）

Bortezomib (PS-341) 是一種可逆性和選擇性的蛋白酶體 (proteasome) 抑制劑，通過靶向蘇氨酸殘基有效抑制 20S 蛋白酶體 (Ki=0.6 nM)。Bortezomib 破壞細胞周期、誘導細胞凋亡以及抑制核因子 NF-κB。Bortezomib 是第一種蛋白酶體抑制劑，具有抗ai活性。

貨號：HY-10227
CAS：179324-69-7

品牌：MCE

型號：HY-10227

起訂量：1

規(guī)格:：5 mg

價格:：￥510

15906629305

在線客服

客服一

上一個

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產品詳情

Bortezomib (Synonyms: 硼替佐米）

Bortezomib (PS-341) 是一種可逆性和選擇性的蛋白酶體 (proteasome) 抑制劑，通過靶向蘇氨酸殘基有效抑制 20S 蛋白酶體 (K_i=0.6 nM)。Bortezomib 破壞細胞周期、誘導細胞凋亡以及抑制核因子 NF-κB。Bortezomib 是第一種蛋白酶體抑制劑，具有抗ai活性。

生物活性

Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (K_i=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^[1]^[2].

IC₅₀ & Target：Ki: 0.6 nM (20S proteasome)

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.

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.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT03117751	St. Jude Children′s Research Hospital\|Incyte Corporation\|Amgen\|Servier	Acute Lymphoblastic Leukemia\|Acute Lymphoblastic Lymphoma	March 29, 2017	Phase 2\|Phase 3
NCT04268199	AHS Cancer Control Alberta\|Tom Baker Cancer Centre	Myeloma\|Myeloma Multiple	May 29, 2020	Phase 2
NCT00006362	Mayo Clinic\|National Cancer Institute (NCI)	Leukemia\|Lymphoma\|Multiple Myeloma and Plasma Cell Neoplasm\|Precancerous Condition\|Unspecified Adult Solid Tumor, Protocol Specific	November 1999	Phase 1

分子量：384.24

Formula：C₁₉H₂₅BN₄O₄

CAS 號：179324-69-7

中文名稱：硼替佐米；保特佐米

運輸條件：Room temperature in continental US; may vary elsewhere.

儲存方式：

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性數據

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

濃度溶劑體積質量	1 mg	5 mg	10 mg

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:

以下溶解方案都請先按照 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儲存條件，適當保存；體內實驗的工作液，建議您現用現配，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沉淀、析出現象，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