853929-59-6

853929-59-6 structure

Name: OGT 2115
Chemical Name: 2-[2-[4-[[1-(4-bromophenyl)-3-oxoprop-1-en-2-yl]amino]-3-fluorophenyl]-1,3-benzoxazol-5-yl]acetic acid
CAS Number: 853929-59-6
Molecular Formula: C₂₄H₁₆BrFN₂O₄
Molecular Weight: 495.297
Catalog: Research Areas Cancer
Create Date: 2017-09-16 06:10:45
Modify Date: 2024-01-30 10:57:15
OGT 2115 is a potent, cell-permeable and orally active heparanase inhibitor with an IC50 of 0.4 μM. OGT 2115 has anti-angiogenic properties (IC50 of 1 μM). OGT 2115 also inhibits heparan sulfate degradation activity[1][2].

Name	2-[2-[4-[[1-(4-bromophenyl)-3-oxoprop-1-en-2-yl]amino]-3-fluorophenyl]-1,3-benzoxazol-5-yl]acetic acid
Synonyms	W-9 hydrochloride [2-(4-{[(2E)-3-(4-Bromophenyl)prop-2-enoyl]amino}-3-fluorophenyl)-1,3-benzoxazol-5-yl]acetic acid [2-(4-{[(2E)-3-(4-Bromophenyl)-2-propenoyl]amino}-3-fluorophenyl)-1,3-benzoxazol-5-yl]acetic acid 5-Benzoxazoleacetic acid, 2-[4-[[(2E)-3-(4-bromophenyl)-1-oxo-2-propen-1-yl]amino]-3-fluorophenyl]- 2-2-4-1-(4-Bromophenyl)-3-oxoprop-1-en-2-ylamino-3-fluorophenyl-1,3-benzoxazol-5-ylacetic acid

Description	OGT 2115 is a potent, cell-permeable and orally active heparanase inhibitor with an IC50 of 0.4 μM. OGT 2115 has anti-angiogenic properties (IC50 of 1 μM). OGT 2115 also inhibits heparan sulfate degradation activity[1][2].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> Others >> Others
Target	IC50: 0.4 μM (Heparanase)[1]
In Vitro	Heparanase InhibitorOGT 2115 can suppress metastasis induced by endoplasmic reticulum (ER) stress in breast cancer cells, although not significantly. However, compared with the control group, the number and rate of migrated cells are significantly reduced following the exposure of the cells to Tunicamycin + OGT 2115. OGT 2115 significantly inhibits the invasion and migration induced by Adriamycin. Furthermore, the MTT assay results show that OGT 2115 does not decrease the anti-proliferative effect of Adriamycin[2].
In Vivo	When administered to mice, OGT 2115 (Compound 12d) shows a plasma concentration of ~10x the heparanase IC50 following oral dosing at 20 mg/kg[1].
References	[1]. [1]Courtney SM, et al. Furanyl-1,3-thiazol-2-yl and benzoxazol-5-yl acetic acid derivatives: novel classes of heparanase inhibitor. Bioorg Med Chem Lett. 2005 May 2;15(9):2295-9. [2]. Li Y, et al. Suppression of endoplasmic reticulum stress-induced invasion and migration of breast cancer cells through the downregulation of heparanase. Int J Mol Med. 2013 May;31(5):1234-42.

Hazard Codes	Xi