IPR-803 - CAS:892243-35-5

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IPR-803

目录号 : KM6059 CAS No. : 892243-35-5 纯度 : 98%

Data Sheet 产品使用指南

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。

规格	价格	是否有货
5mg		In-stock
10mg		In-stock
25mg		In-stock
50mg	询价	In-stock
100mg	询价	In-stock

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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.

体外研究

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

Cell Proliferation Assay

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

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.
IPR-803 has a low oral bioavailability at 4 percent, and remains high concentration even after 10 hours in tumor tissue.
IPR-803 exhibits a half-life (t1/2) of 5 hours.

Animal Model:	NSG mice with MDA-MB-231 cells xenograft
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
Dosage:	200 mg/kg (Pharmacokinetic Study)
Administration:	Oral administration
Result:	t1/2=5 hours.

分子量

453.49

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。