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VERU-111 (Synonyms: VERU-111; ABI-231)

カタログ番号GC37899

VERU-111 (ABI-231) は強力で経口的に活性な α です。および β強力な抗増殖活性を示すチューブリン阻害剤であり、メラノーマおよび前立腺癌細胞株のパネルに対して平均 IC50 は 5.2 nM です。 VERU-111 (ABI-231) は、HPV E6 および E7 を標的とすることにより、子宮頸がん細胞の腫瘍増殖および転移性表現型を抑制し、前立腺がんの治療の可能性を秘めています。

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VERU-111 化学構造

Cas No.: 1332881-26-1

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Sample solution is provided at 25 µL, 10mM.

Description of VERU-111

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]. tubulin[1]

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

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)

[1]. Wang Q, et al. Structure-Guided Design, Synthesis, and Biological Evaluation of (2-(1H-Indol-3-yl)-1H-imidazol-4-yl)(3,4,5-trimethoxyphenyl) Methanone (ABI-231) Analogues Targeting the Colchicine Binding Site in Tubulin. J Med Chem. 2019 Jul 12. [2]. Qinghui Wang, et al. Discovery of ABI-231 analogs targeting the colchicine site in tubulin for advanced melanoma. Cancer Research 76(14 Supplement):4848-4848. [3]. Vivek Kashyap, et al. ABI-231: A novel small molecule suppresses tumor growth and metastatic phenotypes of cervical cancer cells via targeting Human papilloma virus (HPV) E6 and E7. Cancer Research 78(13 Supplement):679-679. [4]. Kashyap VK, et al. Therapeutic efficacy of a novel βIII/βIV-tubulin inhibitor (VERU-111) in pancreatic cancer. J Exp Clin Cancer Res. 2019 Jan 23;38(1):29.

Chemical Properties of VERU-111

Cas No. 1332881-26-1 SDF
同義語 VERU-111; ABI-231
Canonical SMILES O=C(C1=CNC(C2=CNC3=C2C=CC=C3)=N1)C4=CC(OC)=C(OC)C(OC)=C4
Formula C21H19N3O4 M.Wt 377.39
溶解度 Soluble in DMSO Storage 4°C, away from moisture and light
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of VERU-111

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1 mg 5 mg 10 mg
1 mM 2.6498 mL 13.2489 mL 26.4978 mL
5 mM 0.53 mL 2.6498 mL 5.2996 mL
10 mM 0.265 mL 1.3249 mL 2.6498 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 40 reference(s) in Google Scholar.)

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