Ensartinib (X-396) - CAS:1370651-20-9

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Ensartinib (X-396)

目录号 : KG10784 CAS No. : 1370651-20-9 纯度 : 98%

Data Sheet 产品使用指南

Ensartinib (X-396) 是一种能透过血脑屏障的双重 ALK/MET 抑制剂，IC50 分别 <0.4 nM 和 0.74 nM。

规格	价格	是否有货	数量
1mg		In-stock
5mg		In-stock
10mg		In-stock
25mg		In-stock
10 mM * 1 mL in DMSO		In-stock

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Other Forms of Rapamycin:

Ascrinvacumab In-stock
ALK-IN-27 In-stock
Iruplinalkib In-stock
Ensartinib (X-396) In-stock

KKL Med 的所有产品和服务仅用于科学研究，不能被用于人体，兽医，我们也不向个人提供产品和服务。

生物活性

Ensartinib (X-396) is a BBB-permeable and dual ALK/MET inhibitor with IC50s of <0.4 nM and 0.74 nM, respectively.

体外研究

The ability of Ensartinib (X-396) to inhibit the growth of different cancer cell lines harboring ALK fusions or point mutations is tested. Ensartinib is potent in H3122 lung cancer cells harboring EML4-ALK E13;A20 (IC₅₀: 15nM). Ensartinib is also potent in H2228 lung cancer cells harboring EML4-ALK E6a/b; A20 (IC₅₀: 45 nM). Furthermore, X-376 is potent in SUDHL-1 lymphoma cells harboring NPM-ALK (IC₅₀: 9 nM). X-376 also inhibits SY5Y neuroblastoma cells harboring ALK F1174L, MKN-45 gastric carcinoma cells harboring MET dependent, HepG2 cells and PC-9 lung cancer cell lines harboring EGFR exon 19 del with IC₅₀s of 68 nM, 156 nM, 9.644 μM and 2.989 μM, respectively.

体内研究

The effects of Ensartinib (X-396) in vivo against H3122 xenografts are examined. A pharmacokinetic study reveals that Ensartinib shows substantial bioavailability and moderate half-lives in vivo. Nude mice harboring H3122 xenografts are treated with Ensartinib at 25mg/kg bid. Ensartinib significantly delays the growth of tumors compared to vehicle alone. In the xenograft experiments, Ensartinib appears well-tolerated in vivo. Mouse weight is unaffected by Ensartinib treatment. Drug-treated mice appear healthy and do not display any signs of compound related toxicity. To further assess potential side effects of Ensartinib, additional systemic toxicity and toxico-kinetic studies are performed in Sprague Dawley (SD) rats. Following 10 days of repeated oral administration of Ensartinib at 20, 40, 80 mg/kg in SD rats, all animals survive to study termination. The no significant toxicity (NST) levels are determined to be 80mg/kg for Ensartinib. At NST levels, Ensartinib achieves an AUC of 66 μM×hr and a C_max of 7.19 μM.

分子式

C₂₆H₂₇Cl₂FN₆O₃

分子量

561.44

CAS号

1370651-20-9

中文名称

C26H27Cl2FN6O3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 100 mg/mL (178.11 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.7811 mL	8.9057 mL	17.8113 mL
5 mM	0.3562 mL	1.7811 mL	3.5623 mL
10 mM	0.1781 mL	0.8906 mL	1.7811 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。
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。
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。