OGT 2115 

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].

IC50: 0.4 μM (Heparanase)^[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

495.30

Solid

C₂₄H₁₆BrFN₂O₄

853929-59-6

O=C(O)CC1=CC=C(OC(C2=CC=C(NC(/C=C/C3=CC=C(Br)C=C3)=O)C(F)=C2)=N4)C4=C1

Room temperature in continental US; may vary elsewhere.

• [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.  [Content Brief]

  [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.  [Content Brief]