SP-141

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

SP-141  纯度: 99.30%

SP-141 是一种特异性的 MDM2 抑制剂。SP-141 促进 MDM2 自泛素化和降解。SP-141 可用于胰腺癌和乳腺癌的研究。

SP-141

SP-141 Chemical Structure

CAS No. : 1253491-42-7

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 ￥1100 In-stock
5 mg ￥1000 In-stock
10 mg ￥1600 In-stock
25 mg ￥3500 In-stock
50 mg ￥5900 In-stock
100 mg ￥9500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

SP-141 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Anti-Cancer Compound Library
  • Autophagy Compound Library
  • Anti-Aging Compound Library
  • Ferroptosis Compound Library
  • Pyroptosis Compound Library
  • Glutamine Metabolism Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Transcription Factor Targeted Library
  • Anti-Colorectal Cancer Compound Library

生物活性

SP-141 is a specific inhibitor of MDM2. SP-141 promotes MDM2 auto-ubiquitination and degradation. SP-141 might be used for the research of pancreatic cancer and breast cancer cells[1].

IC50 & Target

MDM2[1]
体外研究
(In Vitro)

SP-141 (0.01-10 μM; 72 hours) inhibits human pancreatic cancer cell growth with IC50 values of less than 0.5 μM (0.38-0.50 μM) in a p53-independent manner. The IMR90 cells are much less sensitive to SP141 than the pancreatic cancer cells, suggesting that SP141 has a selective cytotoxicity for cancer cells[1].
SP141 induces MDM2 auto-ubiquitination and proteasomal degradation in both HPAC and Panc-1 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.

Cell Viability Assay[1]

Cell Line: HPAC, Panc-1, AsPC-1, and Mia-Paca-2 pancreatic cancer cell lines. Human primary fibroblasts (IMR90)
Concentration: 0.01, 0.1, 1, and 10 μM
Incubation Time: 72 hours
Result: IC50s of 0.38, 0.50, 0.36, 0.41, and 13.22 μM for HPAC, Panc-1, AsPC-1, Mia-Paca-2, and IMR90, respectively.

Western Blot Analysis[1]

Cell Line: HPAC and Panc-1 cells
Concentration: 0.5 μM
Incubation Time: 120 minutes
Result: Reduced the MDM2 protein levels.
Increased the degradation rate of the MDM2 protein in the presence of Cycloheximide (15 μg/mL).

体内研究
(In Vivo)

SP-141 (40 mg/kg; administered by i.p. injection; 5 d/wk for about three weeks) suppresses pancreatic tumor growth in both xenograft and orthotopic mouse models[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: Nude mice bearing Panc-1 xenograft tumors[1]
Dosage: 40 mg/kg
Administration: Administered by i.p. injection; 5 d/wk for about three weeks
Result: Significantly suppressed the growth of pancreatic xenograft tumors. On Day 18, the tumor volume in the treated group was reduced by 75% compared with that in the control group. There were no significant differences in the body weight compared with the control group.

分子量

324.38

Formula

C22H16N2O
CAS 号

1253491-42-7
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 : 125 mg/mL (385.35 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.0828 mL 15.4140 mL 30.8280 mL
5 mM 0.6166 mL 3.0828 mL 6.1656 mL
10 mM 0.3083 mL 1.5414 mL 3.0828 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: ≥ 2.08 mg/mL (6.41 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (6.41 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% corn oil

    Solubility: ≥ 2.08 mg/mL (6.41 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (6.41 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]. Wei Wang , et al. Identification of a New Class of MDM2 Inhibitor That Inhibits Growth of Orthotopic Pancreatic Tumors in Mice. Gastroenterology. 2014 Oct;147(4):893-902.e2.

    [2]. Wei Wang, et al. The Pyrido[b]indole MDM2 Inhibitor SP-141 Exerts Potent Therapeutic Effects in Breast Cancer Models. Nat Commun. 2014 Oct 1;5:5086.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务