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limertinib
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
limertinib图片
CAS NO:1934259-00-3
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
ASK120067
产品介绍
limertinib (ASK120067) 是一种有效的口服活性EGFRT790M抑制剂 (IC50:0.3 nM),对 EGFRWT(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 ofEGFRT790M(IC50:0.3 nM) with selectivity overEGFRWT(IC50:6.0 nM). limertinib is a third-generation EGFR-TKI for the research of non-small cell lungcancer(NSCLC)[1].

IC50& Target[1]

EGFRT790M

0.5 nM (IC50)

EGFRL858R/T790M

0.3 nM (IC50)

EGFR (WT)

6 nM (IC50)

EGFRExon 19 deletion

0.5 nM (IC50)

体外研究
(In Vitro)

In thein vitrokinase assay limertinib potently inhibits the EGFR L858R/T790M and EGFR T790M resistant mutants with IC50values of 0.3 nM and 0.5 nM, respectively, as well as the EGFRexon19del sensitizing mutant (IC50= 0.5 nM). The50 of limertinib against wild-type EGFR (EGFRWT) is 6 nM[1].
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 (EGFRWT), with IC50 values ranging from 338 nM to 1541 nM[1].
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 (EGFRL858R/T790M) even at low dosage (0.1-1 nM). Additionally, limertinib inhibits p-EGFR and p-Akt and p-erk in EGFR WTA431 cell until the concentration reaches 10 to 100 nM[1].

体内研究
(In Vivo)

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[1].

Animal Model:BALB/cA nude mice[1]
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.
Clinical Trial
分子量

546.06

性状

Solid

Formula

C29H32ClN7O2

CAS 号

1934259-00-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
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 mg5 mg10 mg
1 mM1.8313 mL9.1565 mL18.3130 mL
5 mM0.3663 mL1.8313 mL3.6626 mL
10 mM0.1831 mL0.9157 mL1.8313 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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 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。

*以上所有助溶剂都可在本网站选购。