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

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Sabizabulin (Synonyms: VERU-111; ABI-231) 纯度: 98.02%

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。

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

Sabizabulin Chemical Structure

CAS No. : 1332881-26-1

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50 mg ¥18000 In-stock
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生物活性

VERU-111 (ABI-231) is a potent and orally active 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]

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Clinical Trial

分子量

377.39

Formula

C21H19N3O4

CAS 号

1332881-26-1

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
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 储存时,请在 6 个月内使用,-20°C 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。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in 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 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [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.

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