ASK120067 - CAS:1934259-00-3

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ASK120067

目录号 : KM11145 CAS No. : 1934259-00-3 纯度 : 98%

Data Sheet 产品使用指南

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。ASK120067 是用于非小细胞肺癌 (NSCLC) 研究的第三代 EGFR-TKI。

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10mg		In-stock
25mg		In-stock
50mg		In-stock
100mg		In-stock
200mg	询价	In-stock
500mg	询价	In-stock

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生物活性

ASK120067 is a potent and orally active inhibitor of EGFR (IC₅₀:0.3 nM) with selectivity over EGFR (IC₅₀:6.0 nM). ASK120067 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 ASK120067 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 sensitizing mutant (IC₅₀= 0.5 nM). The ₅₀ of ASK120067 against wild-type EGFR (EGFR) is 6 nM.
ASK120067 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), with IC₅₀ values ranging from 338 nM to 1541 nM.
ASK120067 (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) even at low dosage (0.1-1 nM). Additionally, ASK120067 inhibits p-EGFR and p-Akt and p-erk in EGFR WT A431 cell until the concentration reaches 10 to 100 nM.

体内研究

ASK120067 (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 ASK120067 causes dramatic tumor shrinkage with a TGI rate of 99.3%, exhibiting a similar potency with Osimertinib.

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.

分子量

546.06

CAS号

1934259-00-3

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 : 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。
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。

临床试验

纯度： 98%

Data Sheet

产品使用指南

摩尔计算器
稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度

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浓度

体积

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Other Forms of Rapamycin:

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The molarity calculator equation

The dilution calculator equation