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AZD3759 hydrochloride

产品编号 T4249 CAS 1626387-81-2

AZD3759 hydrochloride 是一种有效的、具有口服活性的中枢神经系统渗透性 EGFR 抑制剂。在 Km ATP 浓度下，EGFR (L858R)/EGFR (wt)/EGFR（外显子 19Del）的 IC50 为 0.2/0.3/0.2 nM。

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AZD3759 hydrochloride Chemical Structure

AZD3759 hydrochloride, CAS 1626387-81-2

规格	价格/CNY	货期
1 mg	￥ 263	现货
2 mg	￥ 369	现货
5 mg	￥ 663	现货
10 mg	￥ 968	现货
25 mg	￥ 1,630	现货
50 mg	￥ 2,900	现货
100 mg	￥ 4,290	现货
500 mg	￥ 9,280	现货
1 mL * 10 mM (in DMSO)	￥ 760	现货

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其他形式的 AZD3759 hydrochloride:

Zorifertinib
现货

选择批次

纯度: 99.41%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	AZD3759 (hydrochloride) is an effective, orally active and central nervous system-penetrant EGFR inhibitor. At Km ATP concentrations, the IC50s are 0.2/0.3/0.2 nM for EGFR (L858R)/EGFR (wt)/EGFR (exon 19Del).
靶点活性	EGFR (WT):0.3nM, EGFR (L858R):0.2nM, EGFR (exon 19Del):0.2 nM
体外活性	At 2 mM of ATP concentrations, the IC50s are 102/7.6/2.4 nM for EGFR (wt)/EGFR (L858R)/EGFR (exon 19Del). AZD3759 also inhibits pEGFR in H838wt (IC50: 64.5 nM), H3255L858R (IC50: 7.2 nM), and PC-9exon 19Del (IC50: 7.4 nM), respectively. In cellular phosphorylation studies, AZD3759 also shows 9-fold inhibition selectivity in EGFR-activating mutant cell lines over EGFR wild-type cell lines (H838 cell line)[1].
体内活性	In rats, absorption of AZD3759 (2 mg/kg, p.o.) is rapid with blood Cmax of 0.58 μM achieved at 1.0 h. And then blood concentrations of AZD3759 decline monoexponentially with a mean elimination half-life of 4.3 h, which is close to the parameter obtained from intravenous dosing of 4.1 h. The bioavailability following an oral dose in rats is 91%. Following the intravenous in dogs, the blood clearance of AZD3759 is 14 mL/min/kg, and the volume of distribution is 6.4 L/kg. Its elimination half-life is 6.2 h. Absorption of AZD3759 is rapid with blood Cmax (698 nM) occurring between 0.5 and 1.5 h. The oral bioavailability of AZD3759 is excellent at 90%. AZD3759 demonstrated significant dose-dependent antitumor efficacy (78% tumor growth inhibition at 7.5 mg/kg/day and tumor regression at 15 mg/kg/day, respectively, 4 weeks after treatment) with <20% body weight loss. AZD3759 (7.5/15 mg/kg) can markedly decrease tumor area. In addition, modulation of pEGFR is detected by a single dose of AZD3759 at 15 mg/kg 1h after dosing[1].
激酶实验	AZD3759 is tested at a single 1 μM concentration across each of 124 kinases from Millipore kinase panel at an ATP concentration that is within 15 μM of their corresponding apparent Km values. In brief, recombinant kinases are incubated within an appropriate buffer containing peptide substrate and radiolabelled γ-33P-ATP together with presence or absence of required inhibitor concentration. The reaction is initiated by adding ATP/Mg2+ mix. After incubation for 40 minutes at room temperature, the reaction is stopped by adding 3% phosphoric acid solution. A portion of reaction mix is spotted onto P30 filter mat to trap peptide and washed three times for 5 minutes with phosphoric acid to remove non-specific γ-33P-ATP. The phosphorylated substrate is then measured by scintillation counting, which determined the level of kinase activity inhibition compared to control reactions[1].
细胞实验	AZD3759 is prepared in DMSO and stored,and then diluted with the appropriate medium before use[1].Cell proliferation assay is determined by MTS methods.Briefly,cells are seeded in 96-well plates (at a density to allow for logarithmic growth during the 72-hour assay) and incubated overnight at 37°C and 5% CO2.Cells are then exposed to concentrations of compounds (e.g.,AZD3759) ranging from 30 mM to 0.3 μM for 72 hours.For the MTS endpoint,cell proliferation is measured by the CellTiter AQueous Non-Radioactive Cell Proliferation Assay reagent.Absorbance is measured with a Tecan Ultra instrument.Predose measurements are made,and concentration needed to reduce the growth of treated cells to half that of untreated cells (GI50) values are determined using absorbance readings[1].
动物实验	AZD3759 is prepared in 1% methylcellulose (Rat)[1].Male Han Wistar rats are orally dosed with the AZD3759 at 2 mg/kg in 1% methylcellulose. At 0.25, 0.5, 1, 2, 4 and 7 hour post-dose, cerebral spinal fluid (CSF) is collected from cisterna magna, and blood samples (>60 μL/time point/each site) are collected via cardiac puncture, into separate EDTA coagulated tubes, and then immediately diluted with 3-fold volume of water. Brain tissue is harvested and homogenized in 3x volume of 100 mM phosphate buffered saline (pH7.4). All samples are stored at -70°C prior to LC/MS/MS analysis.

分子量	496.36
分子式	C22H24Cl2FN5O3
CAS No.	1626387-81-2

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 50 mg/mL (100.73 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0147 mL	10.0733 mL	20.1467 mL	50.3667 mL
	5 mM	0.4029 mL	2.0147 mL	4.0293 mL	10.0733 mL
	10 mM	0.2015 mL	1.0073 mL	2.0147 mL	5.0367 mL
	20 mM	0.1007 mL	0.5037 mL	1.0073 mL	2.5183 mL
	50 mM	0.0403 mL	0.2015 mL	0.4029 mL	1.0073 mL
	100 mM	0.0201 mL	0.1007 mL	0.2015 mL	0.5037 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

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参考文献

1. Zeng Q, et al. Discovery and Evaluation of Clinicalal Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. J Med Chem. 2015 Oct 22;58(20):8200-15.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

AZD3759 hydrochloride 1626387-81-2 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR AZD3759 Hydrochloride AZD-3759 hydrochloride AZD 3759 Hydrochloride AZD-3759 Hydrochloride Inhibitor inhibitor inhibit

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AZD3759 hydrochloride

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords