Xevinapant AT-406; Debio 1143; SM-406|cas:1071992-99-8|西域试剂

Xevinapant AT-406; Debio 1143; SM-406,99.94%

产品编号：Bellancom-15454| CAS NO：1071992-99-8| 分子式：C₃₂H₄₃N₅O₄| 分子量：561.71

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货号	价格	库存与货期
Bellancom-15454	￥1600.00	杭州北京（现货）
Bellancom-15454	￥3500.00	杭州北京（现货）
Bellancom-15454	￥5700.00	杭州北京（现货）

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Xevinapant AT-406; Debio 1143; SM-406

产品介绍

Xevinapant (AT-406) 是一种有效的，可口服的 Smac 模拟物，为 IAPs 的拮抗剂，能够抑制 XIAP，cIAP1 和 cIAP2 蛋白，K_i 值分别为 66.4，1.9 和 5.1 nM。

生物活性

Xevinapant (AT-406) is a potent and orally bioavailable Smac mimetic and an antagonist of IAPs, and it binds to XIAP, cIAP1, and cIAP2 proteins with K_i of 66.4, 1.9, and 5.1 nM, respectively.

体外研究

Xevinapant mimic closely the AVPI peptide in both hydrogen bonding and hydrophobic interactions with XIAP, with additional hydrophobic contacts with W323 of XIAP. Xevinapant is more sensitive to these IAPs than Smac AVPI peptide with 50-100 fold binding affinities. Xevinapant (1 μM) completely restores the activity of caspase-9, which is suppressed by 500 nM XIAP BIR3 in a cell-free system. In MDA-MB-231 cell, Xevinapant induces rapid cellular cIAP1 degradation and also pulls down the cellular XIAP protein. Xevinapant effectively inhibits lots of human cancer cell lines and shows IC₅₀ of 144 and 142 nM in MDA-MB-231 cell and SK-OV-3 ovarian cell, with low toxicity against normal-like human breast epithelial MCF-12F cells and primary human normal prostate epithelial cells. Xevinapant induces apoptosis in MDA-MB-231 cell by inducing activation of caspase-3 and cleavage of PARP. Xevinapant displays single agent activity in ovarian cancer cell lines. The IC₅₀ values of AT-406 in these ovarian cancer cells range from 0.05-0.5 µg/mL. Xevinapant exhibits anti-ovarian cancer efficacy both as a single agent and in combination with carboplatin. Xevinapant (30 μg/mL) induced degradation of XIAP in the drug sensitive ovarian cancer cell lines.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

Xevinapant (AT-406) is very effective in inhibition of tumor growth in the MDA-MB-231 xenograft model, and has minimal toxicity to animals. Xevinapant is evaluated for its pharmacokinetic (PK) properties in mice, rats, non-human primates and dogs.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	SCID mice bearing MDA-MB-231 xenograft tumors
Dosage:	30 and 100 mg/kg
Administration:	p.o.; 5 days a week for 2 weeks
Result:	Strongly inhibits tumor growth at 30 and 100 mg/kg and completely inhibits tumor growth during the treatment with 100 mg/kg.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	SCID mice bearing MDA-MB-231 xenograft tumors
Dosage:	30 and 100 mg/kg
Administration:	p.o.; 5 days a week for 2 weeks
Result:	Strongly inhibits tumor growth at 30 and 100 mg/kg and completely inhibits tumor growth during the treatment with 100 mg/kg.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (178.03 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.7803 mL	8.9014 mL	17.8028 mL
5 mM	0.3561 mL	1.7803 mL	3.5606 mL
10 mM	0.1780 mL	0.8901 mL	1.7803 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 (4.45 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.45 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 (4.45 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.45 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
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (4.45 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.45 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
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玉米油中，混合均匀。