limertinib ASK120067|cas:1934259-00-3|西域试剂

limertinib ASK120067,98.01%

产品编号：Bellancom-138751| CAS NO：1934259-00-3| 分子式：C₂₉H₃₂ClN₇O₂| 分子量：546.06

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货号	价格	库存与货期
Bellancom-138751	￥3000.00	杭州北京（现货）
Bellancom-138751	￥4800.00	杭州北京（现货）
Bellancom-138751	￥9500.00	杭州北京（现货）
Bellancom-138751	￥14500.00	杭州北京（现货）
Bellancom-138751	￥22500.00	杭州北京（现货）

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limertinib ASK120067

产品介绍

limertinib (ASK120067) 是一种有效的口服活性 EGFR^T790M 抑制剂 (IC₅₀:0.3 nM)，对 EGFR^WT(IC₅₀:6.0 nM) 具有选择性。limertinib 是用于非小细胞肺癌 (NSCLC) 研究的第三代 EGFR-TKI。

生物活性

limertinib (ASK120067) is a potent and orally active inhibitor of EGFR^T790M (IC₅₀:0.3 nM) with selectivity over EGFR^WT (IC₅₀:6.0 nM). limertinib is a third-generation EGFR-TKI for the research of non-small cell lung cancer (NSCLC).

体外研究

In the in vitro kinase assay limertinib potently inhibits the EGFR L858R/T790M and EGFR T790M resistant mutants with IC₅₀ values of 0.3 nM and 0.5 nM, respectively, as well as the EGFR^exon19del sensitizing mutant (IC₅₀= 0.5 nM). The ₅₀ of limertinib against wild-type EGFR (EGFR^WT) is 6 nM.
limertinib selectively inhibits the growth of EGFR-mutant cell lines and exhibits potent antiproliferative activity in the mutant EGFR NSCLC cells, with IC₅₀ values of 12 nM, 6 nM and 2 nM against NCI-H1975 (T790M mutation), PC-9, and HCC827 cells (sensitizing mutations), respectively. However, it shows moderate or weak anti-growth activities in A431, LoVo and A549 cells (EGFR^WT), with IC₅₀ values ranging from 338 nM to 1541 nM.
limertinib (0.1-100 nM) inhibits the phosphorylation of EGFR at Tyrosine residue 1068 and its downstream signaling proteins AKT and ERK in NCI-H1975 cells (EGFR^L858R/T790M) even at low dosage (0.1-1 nM). Additionally, limertinib inhibits p-EGFR and p-Akt and p-erk in EGFR WT A431 cell until the concentration reaches 10 to 100 nM.

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

体内研究

limertinib (oral gavage; 5-20 mg/kg; once daily; 21 days) results in significantly regressed tumor growth, with a tumor growth inhibition (TGI) rate of 85.7%, and administration of 10 mg/kg limertinib causes dramatic tumor shrinkage with a TGI rate of 99.3%, exhibiting a similar potency with Osimertinib.

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

Animal Model:	BALB/cA nude mice
Dosage:	5-20 mg/kg
Administration:	Oral gavage; 5-20 mg/kg; once daily; 21 days
Result:	Were well tolerated in animals without observed body weight loss Demonstrated profound and selective antitumor efficacy and decreased TGI rate. Significantly inhibited the phosphorylation of EGFR L858R/T790M and AKT in tumor tissue.

体内研究

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

Animal Model:	BALB/cA nude mice
Dosage:	5-20 mg/kg
Administration:	Oral gavage; 5-20 mg/kg; once daily; 21 days
Result:	Were well tolerated in animals without observed body weight loss Demonstrated profound and selective antitumor efficacy and decreased TGI rate. Significantly inhibited the phosphorylation of EGFR L858R/T790M and AKT in tumor tissue.

性状

Solid

溶解性数据

In Vitro:

DMSO : 41.67 mg/mL (76.31 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8313 mL	9.1565 mL	18.3130 mL
5 mM	0.3663 mL	1.8313 mL	3.6626 mL
10 mM	0.1831 mL	0.9157 mL	1.8313 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 (4.58 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.58 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% corn oil
Solubility: ≥ 2.08 mg/mL (3.81 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.81 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。