| Bioactivity | GW627368 (GW627368X) is a novel, potent and selective competitive antagonist of prostanoid EP4 receptor with additional human TP receptor affinity, with pKi values of 7.0 and 6.8 for human prostanoid EP4 and TP receptors respectively[1]. | ||||||||||||
| Invitro | GW627368 (GW627368X) appears to bind to human prostanoid TP receptors but not the TP receptors of other species[1].GW627368 (GW627368X) (10 μM) produces 100% inhibition of U-46619 (EC100)-induced aggregation (approximate pA2 approximately 7.0) in human washed platelets[1].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[1].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[2]. | ||||||||||||
| 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[3]. Animal Model: | ||||||||||||
| Name | GW627368 | ||||||||||||
| CAS | 439288-66-1 | ||||||||||||
| Formula | C30H28N2O6S | ||||||||||||
| Molar Mass | 544.62 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
|
||||||||||||
| Reference | [1]. Wilson RJ, et al. 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. [2]. Robertson FM, et al. Molecular and pharmacological blockade of the EP4 receptor selectively inhibits both proliferation and invasion of human inflammatory breast cancer cells. J Exp Ther Oncol. 2008;7(4):299-312. [3]. Parida S, et al. 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. |