VERU-111

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

VERU-111 (VERU111) 是微管蛋白中一种新型强效秋水仙碱结合位点抑制剂 (CBSI)，具有潜在的抗癌活性。

VERU-111 (VERU111) is a novel potent colchicine binding site inhibitor (CBSI) in tubulin with potential anticancer activities; inhibits cell viability of human melanoma cell lines (A375, M14, and RPMI7951) with IC50 of 5-10 nM.

VERU-111 (2.5-80 nM; 24-48 hours) inhibits Panc-1, AsPC-1 and HPAF-II cells growth in a dose and time-dependent manner (24 hours: IC50s of 25, 35 and 35?nM, respectively; 48 hours: IC50s of 11.8, 15.5, and 25nM, respectively).VERU-111 (5-20 nM; 24 hours) arrests Panc-1 and AsPC-1 cells in G2/M phase in a dose-dependent manner. VERU-111 (5-20nM; 24 hours) shows dose-dependent inhibition of pro-Caspase 3 and 9 and activation of Caspase-3 and 9, induces the expression of Bax and Bad, and inhibits the expression of Bcl-2 and Bcl-xl proteins in both AsPC-1 and Panc-1 cells. Cell Proliferation Assay Cell Line:Panc-1, AsPC-1, HPAF-II cells Concentration:2.5, 5, 10, 20, 40, 80 nM Incubation Time:24, 48 hours Result:Inhibited the growth of PanCa cells in a dose and time-dependent manner. The IC50 of VERU-111 was 25, 35 and 35?nM in Panc-1, AsPC-1 and HPAF-II, respectively after 24?h treatment, while 48?h post-treatment it was 11.8, 15.5, and 25?nM.Apoptosis AnalysisCell Line:Panc-1, AsPC-1 cells Concentration:5, 10, 20 nM Incubation Time:24 hoursResult:Arrested Panc-1 and AsPC-1 cells in G2/M phase in a dose-dependent manner.Western Blot Analysis Cell Line:AsPC-1 and Panc-1 cells Concentration:5, 10, 20 nM Incubation Time:24 hours Result:Dose-dependent inhibition of pro-Caspase 3 and 9 and activation of Caspase-3 and 9 in both AsPC-1 and Panc-1 cells. Induces the expression of Bax and Bad and inhibited the expression of Bcl-2 and Bcl-xl proteins.

VERU-111 (50μg/mouse; intra-tumorally; 3 times per week for 3weeks) effectively inhibits tumor growth as compared to vehicle-treated group. None of the mouse showed any apparent toxicity as constant increase of body weight in VERU-111 treated mice. Animal Model:Six-week-old female athymic nude mice (bearing AsPC-1 cells)Dosage:50?μg/mouse Administration:Intra-tumorally; 3 times per week for 3?weeks Result:Effectively inhibited tumor growth.

VERU111

Cytoskeleton/Cell Adhesion Molecules

Microtubule/Tubulin

Microtubule/Tubulin

——

——

1332881-26-1

377.4

C21H19N3O4

>98% (HPLC)

In Vitro:?DMSO : 20 mg/mL (53.00 mM)

O=C(C1=CC(OC)=C(OC)C(OC)=C1)C2=CNC(C3=CNC4=CC=CC=C43)=N2

(2-(1H-indol-3-yl)-1H-imidazol-4-yl)(3,4,5-trimethoxyphenyl)methanone

(-20℃)

With Ice Pack

≥ 2 years