生物活性分子抑制剂CUDC-427(Synonyms: GDC-0917)

生物活性分子抑制剂 特异性抑制剂 激动剂 化合物库 重组蛋白 CUDC-427 (Synonyms: GDC-0917) 纯度: 99.01%

CUDC-427 (GDC-0917) 是一种高效的 IAP 抑制剂,常用于各种癌症的研究。

CUDC-427(Synonyms: GDC-0917)

CUDC-427 Chemical Structure

CAS No. : 1446182-94-0

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥2174 In-stock
2 mg ¥1166 In-stock
5 mg ¥1750 In-stock
10 mg ¥2750 In-stock
50 mg ¥7500 In-stock
100 mg   询价  
200 mg   询价  

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CUDC-427 相关产品

相关化合物库:

  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Anti-Cancer Compound Library
  • Clinical Compound Library
  • Anti-Breast Cancer Compound Library

生物活性

CUDC-427 is a potent second-generation pan-selective IAP antagonist, used for treatment of various cancers.

体外研究
(In Vitro)

GDC-0917 (0.1 nM-10 μM) induces reduction of cIAP1 levels in PBMCs in a concentration-dependent manner showing greater than 80% inhibition at concentrations greater than 0.1 µM (56.5 ng/mL)[1].

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.

体内研究
(In Vivo)

GDC-0917 (0.08-16.3 mg/kg) exhibits antitumor activity in a dose dependent manner in the MDA-MB-231-X1.1 Breast Cancer Xenograft, and GDC-0917 is well tolerated, with all dose groups experiencing a <11% decrease in mean body weight. GDC-0917 has low to moderate clearance in the mouse (12.0 mL/min/kg), rat (27.0 mL/min/kg), and dog (15.3 mL/min/kg), and high clearance in the monkey (67.6 mL/min/kg). Oral bioavailability is lowest in monkeys compared with other species[1].

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.

Clinical Trial

分子量

564.70

Formula

C29H36N6O4S

CAS 号

1446182-94-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 100 mg/mL (177.09 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7709 mL 8.8543 mL 17.7085 mL
5 mM 0.3542 mL 1.7709 mL 3.5417 mL
10 mM 0.1771 mL 0.8854 mL 1.7709 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。-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: ≥ 2.5 mg/mL (4.43 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.43 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 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: ≥ 2.5 mg/mL (4.43 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.43 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 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]. Wong H, et al. Learning and confirming with preclinical studies: modeling and simulation in the discovery of GDC-0917, an inhibitor of apoptosis proteins antagonist. Drug Metab Dispos. 2013 Dec;41(12):2104-13.

Animal Administration
[1]

Briefly, 10 million MDA-MB-231-X1.1 breast adenocarcinoma cells resuspended in Hank’s balanced salt solution and Matrigel (1:1, v/v) are implanted subcutaneously into the upper right flank of female SCID.bg mice. MDA-MB-231-X1.1 cells are MDA-MB-231 cells that are selected for improved in vivo growth rates. When tumor volumes reach approximately 100-300 mm3, mice are assigned to treatment groups to get a similar mean tumor size for each treatment group. Treatment groups (n=5 per group) are administered once daily oral doses of vehicle (15% hydroxypropyl-β-cyclodextrin, 20 mM succinic acid in water), 0.08, 0.17, 0.34, 0.68, 1.36, 2.72, 5.43, 10.87, or 16.30 mg/kg of GDC-0917 for 21 days. Tumor volumes are measured in two dimensions (length and width) using Ultra Cal IV calipers. Tumor sizes and body weights are recorded twice weekly, and the mice are regularly observed over the course of the study. Mice are euthanized if their tumor volume exceeds 2000 mm3 or if their body weight drops by more than 20% of the starting weight.

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.

参考文献
  • [1]. Wong H, et al. Learning and confirming with preclinical studies: modeling and simulation in the discovery of GDC-0917, an inhibitor of apoptosis proteins antagonist. Drug Metab Dispos. 2013 Dec;41(12):2104-13.

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