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Sabizabulin
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Sabizabulin图片
CAS NO:1332881-26-1
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品名称
VERU-111
ABI-231
产品介绍
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].

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].

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.
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.
Clinical Trial
分子量

377.39

性状

Solid

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 mg5 mg10 mg
1 mM2.6498 mL13.2489 mL26.4978 mL
5 mM0.5300 mL2.6498 mL5.2996 mL
10 mM0.2650 mL1.3249 mL2.6498 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。

    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-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。

    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本网站选购。