A-385358|cas:406228-55-5|西域试剂

A-385358,98.63%

产品编号：Bellancom-16014| CAS NO：406228-55-5| 分子式：C₃₂H₄₁N₅O₅S₂| 分子量：639.83

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-16014	￥3500.00	杭州北京（现货）
Bellancom-16014	￥5500.00	杭州北京（现货）
Bellancom-16014	￥11000.00	杭州北京（现货）
Bellancom-16014	￥18500.00	杭州北京（现货）
Bellancom-16014	￥28500.00	杭州北京（现货）

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A-385358

产品介绍

A-385358 是 Bcl-X_L 的一个选择性抑制剂，对于 Bcl-X_L 和 Bcl-2 的 K_i 值分别为 0.80 和 67 nM。

生物活性

A-385358 is a selective inhibitor of Bcl-X_L with K_is of 0.80 and 67 nM for Bcl-X_L and Bcl-2, respectively.

体外研究

A-385358 is a selective inhibitor of Bcl-X_L with K_is of 0.80 and 67 nM for Bcl-X_L and Bcl-2, respectively, in fluorescence polarization assays. Treatment of IL-3-deprived FL5.12/Bcl-X_L cells for 24 hours with A-385358 results in cell killing with an EC₅₀ of 0.47±0.05 μM (n=68). This effect is accompanied by an increase in caspase-3 activity. Consistent with the greater affinity for the Bcl-X_L versus Bcl-2 hydrophobic grooves, the EC₅₀ of A-385358 for IL-3-depleted FL5.12/Bcl-2 cells (1.9±0.1 μM; n=55) is 4-fold higher relative to the cytokine-deprived FL5.12/Bcl-X_L cells. In addition, A-385358 is more effective at stimulating cytochrome c release from mitochondria isolated from FL5.12/Bcl-X_L versus Bcl-2 cells.

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

体内研究

The combination of A-385358 given at 100 mg/kg/d plus the lower dose of paclitaxel produces a significant reduction in tumor growth (%T/C) compare with paclitaxel monotherapy. This combination also yields a >100% increase in time for tumors to reach 900 mm³ (%ILS) compare with vehicle control. Maximal efficacy is observed during the dosing period for A-385358, with slow but steady increase in the tumor growth after termination of treatment. The combination of A-385358 at 75 mg/kg/d plus paclitaxel at 30 mg/kg/d is also well tolerated and inhibits tumor growth rate by nearly 80%. Significant effects on tumor growth relative to paclitaxel monotherapy are observed with doses as low as 50 mg/kg/d.

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

体内研究

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

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (78.15 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.5629 mL	7.8146 mL	15.6292 mL
5 mM	0.3126 mL	1.5629 mL	3.1258 mL
10 mM	0.1563 mL	0.7815 mL	1.5629 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 (3.91 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (3.91 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 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 (3.91 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (3.91 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