IPR-803

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IPR-803  纯度: 98.03%

IPR-803 是一种有效的 uPAR•uPA 蛋白-蛋白相互作用 (PPI) 抑制剂。IPR-803 直接与 uPAR 绑定，具有亚微摩尔的亲和力。IPR-803 具有抗肿瘤活性。

IPR-803

IPR-803 Chemical Structure

CAS No. : 892243-35-5

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥3630 In-stock
5 mg ￥3300 In-stock
10 mg ￥5500 In-stock
25 mg ￥9800 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

IPR-803 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Anti-Breast Cancer Compound Library

生物活性

IPR-803 is a potent inhibitor of the uPAR•uPA protein-protein interaction (PPI). IPR-803 binds directly to uPAR with sub-micromolar affinity. IPR-803 displays anti-tumor activity[1].

IC50 & Target

Ki: 0.2 μM (PPI)[1]
体外研究
(In Vitro)

IPR-803 blocks invasion of breast cancer cells line MDA-MB-231, and inhibits matrix metalloproteinase (MMP) breakdown of the extracellular matrix (ECM)[1].
IPR-803 impairs MDA-MB-231 cell adhesion and migration[1].
IPR-803 induces a concentration-dependent impairment of cell adhesion with an IC50 of approximately 30 μM[1].
IPR-803 inhibits MDA-MB-231 cells growth with an IC50 of 58 μM[1].
IPR-803 (0-200 μM; 3 days) blocks the invasion of MDA-MB-231 cells, and most of the inhibition of cell invasion is unlikely due to cytotoxicity of the compound[1].
IPR-803 (1-50 μM; 24 hours) does not have a significant effect on apoptosis or necrosis[1].
IPR-803 (50 μM; 30 minutes) shows inhibition of MAPK phosphorylation[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 Proliferation Assay[1]

Cell Line: MDA-MB-231 cells
Concentration: 0 μM, 50 μM, 150 μM, 200 μM
Incubation Time: 3 days
Result: Displays 90 percent blockage of invasion that is observed at 50 μM.

体内研究
(In Vivo)

IPR-803 (200 mg/kg; i.g.; three times a week; for 5 weeks) impairs breast cancer metastasis, but no statistical significance to the differences in body weight between treated and untreated[1].
IPR-803 has a low oral bioavailability at 4 percent, and remains high concentration even after 10 hours in tumor tissue[1].
IPR-803 exhibits a half-life (t1/2) of 5 hours[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: NSG mice with MDA-MB-231 cells xenograft[1]
Dosage: 200 mg/kg
Administration: Oral gavage; three times a week; for 5 weeks
Result: Impaired metastasis to the lungs.
Animal Model: NOD/SCID mice[1]
Dosage: 200 mg/kg (Pharmacokinetic Study)
Administration: Oral administration
Result: t1/2=5 hours.

分子量

453.49

Formula

C27H23N3O4
CAS 号

892243-35-5
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 : 7.69 mg/mL (16.96 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2051 mL 11.0256 mL 22.0512 mL
5 mM 0.4410 mL 2.2051 mL 4.4102 mL
10 mM 0.2205 mL 1.1026 mL 2.2051 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    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 0.77 mg/mL (1.70 mM); Clear solution

    此方案可获得 ≥ 0.77 mg/mL (1.70 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 7.7 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
*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]. Mani T, et al. Small-molecule inhibition of the uPAR•uPA interaction: synthesis, biochemical, cellular, in vivo pharmacokinetics and efficacy studies in breast cancer metastasis. Bioorg Med Chem. 2013 Apr 1;21(7):2145-55.

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