Bendamustine hydrochloride(Synonyms: 盐酸苯达莫司汀; SDX-105)

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Bendamustine hydrochloride (Synonyms: 盐酸苯达莫司汀; SDX-105) 纯度: 98.94%

Bendamustine hydrochloride (SDX-105),一种嘌呤类似物,是一种 DNA 交联剂。Bendamustine hydrochloride 可激活 DNA 损伤反应和细胞凋亡 (apoptosis)。Bendamustine hydrochloride 具有有效的烷基化,抗癌和抗代谢作用。

Bendamustine hydrochloride(Synonyms: 盐酸苯达莫司汀; SDX-105)

Bendamustine hydrochloride Chemical Structure

CAS No. : 3543-75-7

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥550 In-stock
25 mg ¥500 In-stock
100 mg ¥1548 In-stock
200 mg ¥2418 In-stock
500 mg ¥5200 In-stock
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5 g   询价  

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生物活性

Bendamustine hydrochloride (SDX-105), a purine analogue, is a DNA cross-linking agent. Bendamustine hydrochloride activats DNA-damage stress response and apoptosis. Bendamustine hydrochloride has potent alkylating, anticancer and antimetabolite properties[1].

IC50 & Target

DNA Alkylator/Crosslinker[1]

体外研究
(In Vitro)

Bendamustine is a DNA cross-linking agent that causes DNA breaks, with alkylating and antimetabolite properties. Bendamustine uniquely regulates apoptosis pathways and DNA repair pathways in non-Hodgkin’s lymphoma cells. Bendamustine (50 μM) induces p21 (Cip1/Waf1) and NOXA genes, and increases the expression of p53 in SU-DHL-1 cells. Bendamustine (25 μM) blocks mitotic checkpoints and cuases mitotic catastrophe[1].
Bendamustine reduces the viability of multiple myeloma (MM) cell lines, such as RPMI-8226 and 8226-LR5 cells, with IC25s of 101.8 μM and 585.5 μM after 24 h incubation, and 51.7 and 374.3 μM after 48 h incubation, respectively. Bendamustine induces a specific caspase-dependent MM cell death and inhibits the spindle-assembly checkpoint[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Bendamustine (25 mg/kg, i.v.) shows potent inhibition on the growth of tumor cells by 91%, 99% and 95% for DoHH-2, Granta 519 and RAMOS models, respectively. Moreover, the antitumor effect of Bendamustine is enhanced by rituximab in DoHH-2 and RAMOS models, but not in Granta 519 model[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

394.72

Formula

C16H22Cl3N3O2

CAS 号

3543-75-7

中文名称

盐酸苯达莫司汀

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶解性数据
In Vitro: 

DMSO : 100 mg/mL (253.34 mM; Need ultrasonic)

H2O : 12.5 mg/mL (31.67 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5334 mL 12.6672 mL 25.3344 mL
5 mM 0.5067 mL 2.5334 mL 5.0669 mL
10 mM 0.2533 mL 1.2667 mL 2.5334 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.27 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.27 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (5.27 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.27 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (5.27 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.27 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Leoni LM, et al. Bendamustine (Treanda) displays a distinct pattern of cytotoxicity and unique mechanistic features compared with other alkylating agents. Clin Cancer Res. 2008 Jan 1;14(1):309-17.

    [2]. Cives M, et al. Bendamustine overcomes resistance to melphalan in myeloma cell lines by inducing cell death through mitotic catastrophe. Cell Signal. 2013 May;25(5):1108-17.

    [3]. Ackler S, et al. Navitoclax (ABT-263) and bendamustine ± rituximab induce enhanced killing of non-Hodgkin’s lymphoma tumours in vivo. Br J Pharmacol. 2012 Oct;167(4):881-91.

Cell Assay
[2]

Cytotoxicity of both Bendamustine and melphalan on multiple myeloma (MM) cells is calculated as inhibition of cell viability by measuring the percentage of cell survival by MTS assay. Briefly, cells (1 × 104/well) are seeded in 96-well plates with increasing concentrations of the drug and analyzed after 24, 48, 72 and 96 h of incubation. To this end, 1 μg/mL of MTS solution is added to each well and, after 1 h at 37 °C, the dark blue formazan crystals are dissolved by isopropanol 1 N and HCl (24:1, vol/vol). Finally, the absorbance is measured at 490 nm in a 96-well plate reader. Cell survival is estimated as the percentage of the absorbance of untreated controls and each test is performed in triplicate. The inhibitory concentrations 50 (IC50) and 25 (IC25) of each drug, being the amount able to reduce cell growth to 50% and 25%, respectively, of that of untreated control cells, are calculated, and the tests are performed in parallel using equitoxic concentrations of Bendamustine and melphalan. The relative resistance index (RRI) is expressed as the ratio of the IC50 of 8226-LR5 to the IC50 of RPMI-8226 cells[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[3]

Mice[3]
C.B.-17 scid mice (DoHH-2, Granta 519) or C.B.-17 scid-bg mice (SuDHL-4, RAMOS) are inoculated with 1 × 106 (DoHH-2, RAMOS), 3 × 106 (SuDHL-4) or 5 × 106 (Granta 519) cells s.c. in the right flank. For flank xenografts, inoculation volume is 0.2 mL consisting of a 50:50 mixture of cells in growth medium and Matrigel. Tumour volume is estimated by two to three weekly measurements of the length and width of the tumour by electronic calipers and applying the following equation: V=L×W2/2. Tumours are allowed to reach approximately 250 mm3, and mice are size-matched (day 0) into treatment and control groups. For systemic Granta 519 tumour models, 2 × 106 cells are injected via the tail vein in 0.1 mL volume of cell medium on day 0, and treatment is initiated on day 14. All animals are ear-tagged and monitored individually throughout the experiment. Navitoclax is administered by oral gavage once daily in a mixture of Phosal 50PG : PEG400 : ethanol. Bendamustine and rituximab are administered i.v. at 25 mg/kg and 10 mg/kg, respectively, on day 1. Navitoclax is administered approximately 2 h before Bendamustine and rituximab. All trials are comprised of 10 mice per group. Mice are humanely killed when tumours reach a size >2000 mm3 or when any signs of distress are monitored. Signs of distress include loss of ambulation, laboured breathing or weight loss > 20% mean body weight per cage[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. Leoni LM, et al. Bendamustine (Treanda) displays a distinct pattern of cytotoxicity and unique mechanistic features compared with other alkylating agents. Clin Cancer Res. 2008 Jan 1;14(1):309-17.

    [2]. Cives M, et al. Bendamustine overcomes resistance to melphalan in myeloma cell lines by inducing cell death through mitotic catastrophe. Cell Signal. 2013 May;25(5):1108-17.

    [3]. Ackler S, et al. Navitoclax (ABT-263) and bendamustine ± rituximab induce enhanced killing of non-Hodgkin’s lymphoma tumours in vivo. Br J Pharmacol. 2012 Oct;167(4):881-91.

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