IPR-803


Catalog No. Size PriceQuantity
M23941-C Contact sales@xcessbio.com for quotation $100Unavailable

Description

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.

Product information

CAS Number: 892243-35-5

Molecular Weight: 453.49

Formula: C27H23N3O4

Chemical Name: 3-{[12-(azepan-1-yl)-8-oxo-15-oxa-14-azatetracyclo[7.6.1.0²,⁷.0¹³,¹⁶]hexadeca-1(16),2,4,6,9,11,13-heptaen-10-yl]amino}benzoic acid

Smiles: OC(=O)C1=CC(=CC=C1)NC1C=C(C2=NOC3=C2C=1C(=O)C1=CC=CC=C31)N1CCCCCC1

InChiKey: UAEULQWANHYLGJ-UHFFFAOYSA-N

InChi: InChI=1S/C27H23N3O4/c31-25-18-10-3-4-11-19(18)26-23-22(25)20(28-17-9-7-8-16(14-17)27(32)33)15-21(24(23)29-34-26)30-12-5-1-2-6-13-30/h3-4,7-11,14-15,28H,1-2,5-6,12-13H2,(H,32,33)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 7.69 mg/mL (16.96 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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). 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.

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. 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.

Products are for research use only. Not for human use.

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