GW-627368X

GW-627368X is a novel, potent and selective competitive antagonist of prostanoid EP4 receptors with additional human TP receptor affinity. Oral administration of GW627368X showed significant tumor regression characterized by tumor reduction and induction of apoptosis. Reduction in prostaglandin E2 synthesis also led to reduced level of VEGF in plasma. GW627368X will be a valuable tool to explore the role of the prostanoid EP4 receptor in many physiological and pathological settings.

Product information

CAS Number: 439288-66-1

Molecular Weight: 544.62

Formula: C30H28N2O6S

Synonym:

GW627368X

GW 627368X

GW-627368

GW 627368

GW627368

GW-627368X

Chemical Name: 2-(4-(4,9-diethoxy-1-oxo-1,3-dihydro-2H-benzo[f]isoindol-2-yl)phenyl)-N-(phenylsulfonyl)acetamide

Smiles: CCOC1=C2C=CC=CC2=C(OCC)C2=C1CN(C1=CC=C(CC(=O)NS(=O)(=O)C3C=CC=CC=3)C=C1)C2=O

InChiKey: XREWXJVMYAXCJV-UHFFFAOYSA-N

InChi: InChI=1S/C30H28N2O6S/c1-3-37-28-23-12-8-9-13-24(23)29(38-4-2)27-25(28)19-32(30(27)34)21-16-14-20(15-17-21)18-26(33)31-39(35,36)22-10-6-5-7-11-22/h5-17H,3-4,18-19H2,1-2H3,(H,31,33)

Technical Data

Appearance: Solid Power.

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

Solubility: Soluble in DMSO, not in water

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:

GW627368 (GW627368X) appears to bind to human prostanoid TP receptors but not the TP receptors of other species. GW627368 (GW627368X) (10 μM) produces 100% inhibition of U-46619 (EC100)-induced aggregation (approximate pA2 approximately 7.0) in human washed platelets. GW627368 (GW627368X) is devoid of agonist activity and actually produced a significant and concentration-related reduction in basal cAMP levels with pIC50 value of 6.3. GW627368 (GW627368X) induces inhibition of proliferation and invasion of human SUM149 IBC tumor cells beginning at 0.1 μM, with inhibition of proliferation and invasion of MDA-MB-231 non-IBC cells at higher concentrations.

In Vivo:

GW627368 (GW627368X) (0-15 mg/kg; p.o.; every alternate day for 28 days) shows significant tumor regression characterized by tumor reduction and induction of apoptosis.

References:

1. Parida S, Parekh A, Dey G, Ghosh SC, Mandal M. Molecular inhibition of prostaglandin E2 with GW627368X: Therapeutic potential and preclinical safety assessment in mouse sarcoma model. Cancer Biol Ther. 2015;16(6):922-32. doi: 10.1080/15384047.2015.1040953. Epub 2015 Apr 20. PubMed PMID: 25894216.
2. Wilson RJ, Giblin GM, Roomans S, Rhodes SA, Cartwright KA, Shield VJ, Brown J, Wise A, Chowdhury J, Pritchard S, Coote J, Noel LS, Kenakin T, Burns-Kurtis CL, Morrison V, Gray DW, Giles H. GW627368X ((N-{2-[4-(4,9-diethoxy-1-oxo-1,3-dihydro-2H-benzo[f]isoindol-2-yl)phenyl]acetyl} benzene sulphonamide): a novel, potent and selective prostanoid EP4 receptor antagonist. Br J Pharmacol. 2006 Jun;148(3):326-39. PubMed PMID: 16604093; PubMed Central PMCID: PMC1751567.

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