DI-87|cas:2107280-55-5|西域试剂

DI-87,98.97%

产品编号：Bellancom-133141| CAS NO：2107280-55-5| 分子式：C₂₃H₃₀N₆O₃S₂| 分子量：502.65

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	包装	价格	库存与货期	购买量	操作
Bellancom-133141		￥8500.00	杭州北京（现货）
Bellancom-133141		￥14500.00	杭州北京（现货）

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DI-87

产品介绍

DI-87 是一种具有口服活性的，选择性的脱氧胞苷激酶 (dCK) 抑制剂，EC₅₀ 为 10.2 nM。DI-87 具有抗肿瘤活性，可通过联合用药来抑制表达 dCK 的肿瘤。

生物活性

DI-87 is an orally active and selective deoxycytidine kinase (dCK) inhibitor with an EC₅₀ of 10.2 nM. DI-87 has antitumor activity and is used in combination therapy against tumors expressing dCK.

体外研究

(S)-DI-87 exhibits a much higher IC₅₀ value (IC₅₀=468 nM) relative to DI-87 ((R)-DI-8) (IC₅₀=3.15 nM) in CEM T-ALL cells for inhibition of dCK activity.
DI-87 (1 µM; for 72 hours) rescues human cell line CCRF-CEM (CEM) cells from the anti-proliferative effects of gemcitabine, a dCK-dependent nucleoside analog prodrug, with an EC₅₀ of 10.2 nM.

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

体内研究

DI-87 (5-25 mg/kg; oral gavage) exhibits full dCK inhibition for 27 hours, and enzyme activity fully recovered by 36 hours with 25 mg/kg dose.
DI-87 (10-50 mg/kg; oral) has plasma concentrations of between 1 and 3 hours and plasma half-life of 4 hours.
DI-87 (10 mg/kg/day or 25 mg/kg/twice a day; oral; for 16-18 days) with thymidine (2 g/kg; ip; twice a day) results in reduced tumor growth in male NSG mice implanted with CEM tumors.

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

Animal Model:	8-12 week-old male or female NSG mice with CEM tumor xenografts
Dosage:	5, 10, 25 mg/kg
Administration:	Oral gavage
Result:	The 25 mg/kg dose exhibited full dCK inhibition for 27 hours, and enzyme activity fully recovered by 36 hours. The 10 mg/kg dose resulted in full inhibition with recovery initiating at the 12 hours time point. The 5 mg/kg dose resulted in minimal dCK inhibition with rapid recovery.

Animal Model:	Female NSG mice with CEM tumors
Dosage:	10, 25, or 50 mg/kg
Administration:	Oral
Result:	Had plasma concentrations of between 1 and 3 hours and plasma half-life of 4 hours. Had tumor concentrations lower than plasma and had a later, more sustained peak at 3-9 hours.

体内研究

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

Animal Model:	8-12 week-old male or female NSG mice with CEM tumor xenografts
Dosage:	5, 10, 25 mg/kg
Administration:	Oral gavage
Result:	The 25 mg/kg dose exhibited full dCK inhibition for 27 hours, and enzyme activity fully recovered by 36 hours. The 10 mg/kg dose resulted in full inhibition with recovery initiating at the 12 hours time point. The 5 mg/kg dose resulted in minimal dCK inhibition with rapid recovery.

Animal Model:	Female NSG mice with CEM tumors
Dosage:	10, 25, or 50 mg/kg
Administration:	Oral
Result:	Had plasma concentrations of between 1 and 3 hours and plasma half-life of 4 hours. Had tumor concentrations lower than plasma and had a later, more sustained peak at 3-9 hours.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (198.95 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9895 mL	9.9473 mL	19.8946 mL
5 mM	0.3979 mL	1.9895 mL	3.9789 mL
10 mM	0.1989 mL	0.9947 mL	1.9895 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 (4.97 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.97 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 (4.97 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (4.97 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 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 (4.97 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.97 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。