CRT0273750|cas:1979939-16-6|西域试剂

CRT0273750,98.72%

产品编号：Bellancom-120797| CAS NO：1979939-16-6| 分子式：C₂₅H₂₂ClF₃N₄O₂| 分子量：502.92

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-120797	￥1500.00	杭州北京（现货）
Bellancom-120797	￥2400.00	杭州北京（现货）
Bellancom-120797	￥5400.00	杭州北京（现货）
Bellancom-120797	￥9200.00	杭州北京（现货）
Bellancom-120797	￥16000.00	杭州北京（现货）

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CRT0273750

产品介绍

CRT0273750 是 ATX 抑制剂的先导化合物，并调节血浆中 LPA 水平。CRT0273750 可用于 ATX/LPA 依赖性癌症模型。

生物活性

CRT0273750 is an autotaxin (ATX) inhibitor and modulates LPA levels in plasm (IC₅₀ = 0.014 μM). CRT0273750 can be used in ATX/LPA-dependent models of cancer.

体外研究

CRT0273750 shows high potency in both the biochemical (IC₅₀ = 0.01 μM) and plasma choline release assay(IC₅₀ = 0.014 μM).
CRT0273750 is also shown to inhibit the migration of 4T1 cells with an EC50 of 0.025μM.

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

体内研究

CRT0273750 (1 mg/kg; i.v.)has a moderate blood clearance, with value of 41 mL/min/kg.
CRT0273750 (10 mg/kg; oral administration) treatment shows the C_max, AUC and t_1/2 values of 3.8 µM, 3.2 µM.h and 1.4 h, respectively.
CRT0273750 (10, 30 and 100 mg/kg; oral administration) shows a proportional increase.

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

Animal Model:	CD-1 mice
Dosage:	1 mg/kg
Administration:	I.v.
Result:	Had a moderate blood clearance.

Animal Model:	Balb-c nu/nu mice
Dosage:	10, 30 and 100 mg/kg
Administration:	Oral administration (Pharmacokinetic Analysis)
Result:	The C_maxs were 3.8, 10.9 and 18.1 µM, respectively. The AUCs were 3.2, 15.2 and 59.3 µM.h, respectively. The t_1/2s were 1.4, 0.9 and 1.3 h, respectively.

体内研究

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

Animal Model:	CD-1 mice
Dosage:	1 mg/kg
Administration:	I.v.
Result:	Had a moderate blood clearance.

Animal Model:	Balb-c nu/nu mice
Dosage:	10, 30 and 100 mg/kg
Administration:	Oral administration (Pharmacokinetic Analysis)
Result:	The C_maxs were 3.8, 10.9 and 18.1 µM, respectively. The AUCs were 3.2, 15.2 and 59.3 µM.h, respectively. The t_1/2s were 1.4, 0.9 and 1.3 h, respectively.

性状

Solid

溶解性数据

In Vitro:

DMSO : 250 mg/mL (497.10 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9884 mL	9.9419 mL	19.8839 mL
5 mM	0.3977 mL	1.9884 mL	3.9768 mL
10 mM	0.1988 mL	0.9942 mL	1.9884 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: ≥ 2.08 mg/mL (4.14 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.14 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
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (4.14 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.14 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。