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產(chǎn)地	進(jìn)口	級(jí)別	其他

注：本產(chǎn)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(gè)可逆的和有選擇性的蛋白酶體抑制劑,20年代,強(qiáng)有力地抑制蛋白酶體(Ki = 0.6海里)通過(guò)瞄準(zhǔn)一個(gè)threonine殘基。Bortezomib干擾細(xì)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.

體內(nèi)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.

分子量

384.24

性狀

Solid

Formula

C₁₉H₂₅BN₄O₄

CAS 號(hào)

179324-69-7

中文名稱(chēng)

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)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(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(chǔ)備液

濃度溶劑體積質(zhì)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(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?6 個(gè)月內(nèi)使用，-20°C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?1 個(gè)月內(nèi)使用。

In Vivo:

請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥方式選擇適當(dāng)?shù)娜芙夥桨?。以下溶解方案都?qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：

——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶

1.

請(qǐng)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(qǐng)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(qǐng)依序添加每種溶劑： 10% EtOH 90% corn oil
Solubility: ≥ 4 mg/mL (10.41 mM); Clear solution
4.

請(qǐng)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(qǐng)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(qǐng)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(qǐng)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(qǐng)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(qǐng)依序添加每種溶劑： 1% DMSO 99% saline
Solubility: ≥ 0.5 mg/mL (1.30 mM); Clear solution