VERU-111 (ABI-231) 是一种高效、口服可利用 α/β 微管蛋白(tubulin)抑制剂，具有很强的抗增殖活性，对黑素瘤和前列腺癌细胞系作用的平均 IC50值为 5.2 nM。VERU-111 (ABI-231) 通过靶向 HPV E6 和 E7 抑制肿瘤生长和转移表型，有潜力用于前列腺癌的研究。
| 生物活性 | VERU-111 (ABI-231) is a potent and orally activeα and β tubulininhibitor, which displays strong antiproliferative activity, with an average IC50of 5.2 nM against panels of melanoma and prostatecancercell lines. VERU-111 (ABI-231) suppresses tumor growth and metastatic phenotypes of cervicalcancercells via targetingHPVE6 and E7, and has potential for the treatment of prostatecancer[1][2][3]. |
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体外研究
(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 IC50of 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. |
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体内研究
(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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light) |
| 溶解性数据 | In Vitro: DMSO : 20 mg/mL(53.00 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.6498 mL | 13.2489 mL | 26.4978 mL | | 5 mM | 0.5300 mL | 2.6498 mL | 5.2996 mL | | 10 mM | 0.2650 mL | 1.3249 mL | 2.6498 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture and light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2 mg/mL (5.30 mM); Clear solution
此方案可获得 ≥ 2 mg/mL (5.30 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: 2 mg/mL (5.30 mM); Suspended solution; Need ultrasonic
此方案可获得 2 mg/mL (5.30 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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