1. Cell Cycle/DNA Damage
    Cytoskeleton
  2. Microtubule/Tubulin
  3. VERU-111

VERU-111 (Synonyms: ABI-231)

Cat. No.: HY-120599
Handling Instructions

VERU-111 (ABI-231) is a potent and orally bioavailable α and β tubulin inhibitor, which displays strong antiproliferative activity, with an average IC50 of 5.2 nM against panels of melanoma and prostate cancer cell lines. VERU-111 (ABI-231) suppresses tumor growth and metastatic phenotypes of cervical cancer cells via targeting HPV E6 and E7, and has potential for the treatment of prostate cancer.

For research use only. We do not sell to patients.

VERU-111 Chemical Structure

VERU-111 Chemical Structure

CAS No. : 1332881-26-1

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Description

VERU-111 (ABI-231) is a potent and orally bioavailable α and β tubulin inhibitor, which displays strong antiproliferative activity, with an average IC50 of 5.2 nM against panels of melanoma and prostate cancer cell lines. VERU-111 (ABI-231) suppresses tumor growth and metastatic phenotypes of cervical cancer cells via targeting HPV E6 and E7, and has potential for the treatment of prostate cancer[1][2][3].

IC50 & Target

tubulin[1]

In Vitro

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 25 nM, respectively)[4].
VERU-111 (5-20 nM; 24 hours) arrests Panc-1 and AsPC-1 cells in G2/M phase in a dose-dependent manner[4].
VERU-111 (5-20 nM; 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[4].

Cell Proliferation Assay[4]

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 Analysis[4]

Cell Line: Panc-1, AsPC-1 cells
Concentration: 5, 10, 20 nM
Incubation Time: 24 hours
Result: Arrested Panc-1 and AsPC-1 cells in G2/M phase in a dose-dependent manner.

Western Blot Analysis[4]

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.
In Vivo

VERU-111 (50 μg/mouse; intra-tumorally; 3 times per week for 3 weeks) 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[4].

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.
Molecular Weight

377.39

Formula

C₂₁H₁₉N₃O₄

CAS No.

1332881-26-1

SMILES

O=C(C1=CNC(C2=CNC3=C2C=CC=C3)=N1)C4=CC(OC)=C(OC)C(OC)=C4

Shipping

Room temperature in continental US; may vary elsewhere

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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