Methanone, [2-(1H-indol-3-yl)-1H-imidazol-5-yl](3,4,5-trimethoxyphenyl)- Chemical Properties

Boiling point:

688.1±55.0 °C(Predicted)

Density 

1.306±0.06 g/cm3(Predicted)

storage temp. 

4°C, away from moisture and light

solubility 

Soluble in DMSO

pka

10.82±0.10(Predicted)

form 

Solid

color 

Light yellow to yellow

Methanone, [2-(1H-indol-3-yl)-1H-imidazol-5-yl](3,4,5-trimethoxyphenyl)- Usage And Synthesis

Description

Sabizabulin (VERU-111) is a potent, orally bioavailable, and well-tolerated microtubule inhibitor that Veru Inc. is currently developing. It can inhibit the growth of ovarian tumors and completely suppress tumor metastasis in vivo, with efficacy comparable to that of paclitaxel, the current first-line treatment for ovarian cancer. VERU-111 can block the polymerization of tubulin and is not a substrate for multi-drug resistance mechanisms.

in vitro

In vitro experiments have shown that VERU-111 has a significant inhibitory effect on the ovarian cancer cell lines SKOV3 and OVCAR3. It can effectively inhibit colony formation, proliferation, invasion, and migration of cells at nanomolar levels. In addition, VERU-111 can induce apoptosis in a concentration-dependent manner, with an effect comparable to that of the standard chemotherapeutic drug paclitaxel.

in vivo

In vivo experiments have also shown VERU-111 to have strong anti-tumor and anti-metastatic activity. In a mouse model with orthotopic transplantation of SKOV3 ovarian cancer tumor cells, VERU-111 significantly inhibited tumor growth and completely blocked tumor metastasis to distant organs. Importantly, VERU-111 showed good tolerability during the treatment process, without systemic toxicity.

Clinical claims and research

Sabizabulin has entered Phase II clinical trials for the treatment of ER+ HER2- metastatic breast cancer (NCT05079360), Phase III clinical trials for the treatment of metastatic castration-resistant prostate cancer (mCRPC) (NCT04844749), and Phase III clinical trials for the treatment of COVID-19 (NCT04842747).