IPR-803 是一种有效的 uPARouPA 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。
| 生物活性 | IPR-803 is a potent inhibitor of theuPARouPA protein-protein interaction (PPI). IPR-803 binds directly to uPAR with sub-micromolar affinity. IPR-803 displays anti-tumor activity[1]. |
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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 IC50of approximately 30 μM[1].
IPR-803 inhibits MDA-MB-231 cells growth with an IC50of 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].
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. |
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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].
| 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. |
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| 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 |
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| 溶解性数据 | In Vitro: DMSO : 7.69 mg/mL(16.96 mM;Need ultrasonic) 配制储备液 | 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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 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-CDin 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 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
*以上所有助溶剂都可在本网站选购。 |
