MCB-613

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MCB-613  纯度: 99.95%

MCB-613 是一种有效的类固醇受体共激活因子 (SRC) 小分子“刺激物” (SMS)，超刺激 SRCs 的转录活性。 MCB-613 增加了 SRC 与其他共激活因子的相互作用，并显着诱导 ER 应激与活性氧 (ROS) 的产生相结合。 MCB-613 是一种 SMS，通过过度刺激 SRC 致癌程序，靶向癌基因用作抗癌药物。

MCB-613

MCB-613 Chemical Structure

CAS No. : 1162656-22-5

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 ￥1210 In-stock
5 mg ￥1100 In-stock
10 mg ￥1900 In-stock
25 mg ￥3900 In-stock
50 mg ￥6200 In-stock
100 mg ￥9900 In-stock
200 mg   询价  
500 mg   询价  

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MCB-613 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Anti-Cancer Compound Library
  • Endoplasmic Reticulum Stress Compound Library

生物活性

MCB-613 is a potent Steroid receptor coactivator SRC small molecule ‘stimulator’ (SMS), super-stimulates SRCs’ transcriptional activity. MCB-613 increases SRCs’ interactions with other coactivators and markedly induces ER stress coupled to the generation of reactive oxygen species (ROS). MCB-613 is a SMS that target oncogenes can be exploited as anti-cancer agents by over-stimulating the SRC oncogenic program[1].

体外研究
(In Vitro)

MCB-613 (6-8 μM; 24 hours) activates endogenous MMP13 mRNA expression in MDA-MB-231 cells[1].
MCB-613 (2-10 μM; 4 hours) leads to proteasome dysfunction and ER stress, the induction of the markers for unfolded protein response (UPR), including the phosphorylation of eIF2α and IRE1α as well as the induction of ATF4 protein expression[1].
MCB-613 (0-7 μM; 4 hours) affects SRC-3 KO and WT HeLa cell viability, SRC-3 WT HeLa cell is more affected by MCB-613 compared with KO cells[1].

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.

RT-PCR[1]

Cell Line: MDA-MB-231 cells
Concentration: 6 μM; 8 μM
Incubation Time: 24 hours
Result: Increased MMP13 mRNA expression.

Western Blot Analysis[1]

Cell Line: HeLa cells
Concentration: 2 μM; 4 μM; 6 μM; 8 μM; 10 μM
Incubation Time: 24 hours
Result: Induced the p-eIF2α, p-IRE1α, and ATF-4 protein expression.

Cell Viability Assay[1]

Cell Line: SRC-3 KO and WT HeLa cells
Concentration: 3 μM; 4 μM; 5 μM; 6 μM; 7 μM
Incubation Time: 24 hours
Result: Decreased SRC-3 KO and WT HeLa cell viability.

体内研究
(In Vivo)

MCB-613 (intravenous injection; 20 mg/kg; 3 times/week; 7 weeks) significantly and dramatically stalls the growth of the tumor compared with the control group and causes no obvious animal toxicity[1]

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 Model: MCF-7 breast cancer mouse xenograft model (athymic nude mice by injecting MCF-7 cells into mammary fat pads)[1]
Dosage: 20 mg/kg
Administration: Intravenous injection; 20 mg/kg; 3 times/week; 7 weeks
Result: Inhibited tumor growth in vivo.

分子量

304.39

Formula

C20H20N2O
CAS 号

1162656-22-5
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 50 mg/mL (164.26 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.2853 mL 16.4263 mL 32.8526 mL
5 mM 0.6571 mL 3.2853 mL 6.5705 mL
10 mM 0.3285 mL 1.6426 mL 3.2853 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。-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: ≥ 2.5 mg/mL (8.21 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.21 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 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: ≥ 2.5 mg/mL (8.21 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.21 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 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: ≥ 2.5 mg/mL (8.21 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.21 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 25.0 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]. Wang L, et al. Characterization of a Steroid Receptor Coactivator Small Molecule Stimulator that Overstimulates Cancer Cells and Leads to Cell Stress and Death. Cancer Cell. 2015 Aug 10;28(2):240-52.

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