AZD3965|cas:1448671-31-5|西域试剂

AZD3965,99.86%

产品编号：Bellancom-12750| CAS NO：1448671-31-5| 分子式：C₂₁H₂₄F₃N₅O₅S| 分子量：515.51

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-12750	￥990.00	杭州北京（现货）
Bellancom-12750	￥1500.00	杭州北京（现货）
Bellancom-12750	￥2400.00	杭州北京（现货）
Bellancom-12750	￥7800.00	杭州北京（现货）
Bellancom-12750	￥13000.00	杭州北京（现货）

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AZD3965

产品介绍

AZD3965是选择性的 MCT1 抑制剂，K_i 值为1.6 nM，比MCT2的选择性高6倍。

生物活性

AZD3965 is a selective MCT1 inhibitor with a K_i of 1.6 nM, showing 6-fold selectivity over MCT2.

体外研究

AZD3965 is designed to selectively inhibit Monocarboxylate transporter-1 (MCT1) and will therefore be expected to influence the movement of lactate into and out of cells. AZD3965 treatment causes a 3.7 fold increase in intracellular lactate in hypoxic COR-L103 and 3.7 fold and 3.9 fold increases in normoxic and hypoxic NCI-H1048 cells respectively. In all other cases a <1.9 fold increase is observed. These data are consistent with AZD3965 blocking lactate transport in cells where AZD3965 also reduces cell number and is consistent with AZD3965 acting via inhibition of MCT1. When MCT1 is overexpressed the EC₅₀ of NCI-H1048 is increased from 0.14 nM to 10.5 nM in NCI-H1048 cells. This is consistent with AZD3965 acting via MCT1 inhibition.

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

体内研究

COR-L103 tumor bearing mice are treated with 100 mg/kg AZD3965 or vehicle BIDfor 21 days and the tumor volume monitored. Pharmacokinetic analysis demonstrates that 100 mg/kg AZD3965 BID results in concentrations of free AZD3965 predicted to inhibit lactate transport. AZD3965 treatment significantly reduces the growth of COR-L103 tumors, although tumor regression is not seen, consistent with AZD3965 only targeting the hypoxic fraction of the tumor.

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 : 100 mg/mL (193.98 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9398 mL	9.6991 mL	19.3983 mL
5 mM	0.3880 mL	1.9398 mL	3.8797 mL
10 mM	0.1940 mL	0.9699 mL	1.9398 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： 0.5% HPMC 0.2%Tween80
Solubility: 5 mg/mL (9.70 mM); Suspended solution; Need ultrasonic
2.

请依序添加每种溶剂： 20% HP-β-CD in saline
Solubility: 5 mg/mL (9.70 mM); Suspended solution; Need ultrasonic and warming and heat to 60°C
3.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (4.03 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.03 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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
4.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (4.03 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.03 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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
5.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (4.03 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.03 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。