AZD3759|EGFR|for research only|Ambeed

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AZD3759 98%

货号：A171107 产品仅供科研

AZD3759 is an inhibitor of EGFR (WT), EGFR (L858R) and EGFR (exon 19 deletion) (IC50s values are 0.3 nM, 0.2 nM and 0.2 nM, respectively).

AZD3759 化学结构
CAS号：1626387-80-1

AZD3759 3D分子结构
CAS号：1626387-80-1

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AZD3759 纯度/质量文件

货号：A171107 标准纯度：98% 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Mar. Drugs,2024,22(5):194. Ambeed. [ A104599 ]; • Pharmaceuticals,2024,17(5):570. Ambeed. [ A224421 ]; 更多 >

EGFR 亚型比较

产品名称	EGFR/ErbB1 ↓ ↑	ErbB3 ↓ ↑	ErbB4 ↓ ↑	HER2/ErbB2 ↓ ↑	mutant EGFR ↓ ↑	其他靶点	纯度
WZ-3146	++++ EGFR (E746_A750), IC50: 2 nM EGFR (E746_A750/T790M), IC50: 14 nM						99%+
Daphnetin	+ EGFR, IC50: 7.67 μM					PKC,PKA	95%
Lifirafenib	++ EGFR, IC50: 29 nM				+ EGFR(T790M/L858R), IC50: 495 nM		96%
PD168393	++++ EGFR, IC50: 0.70 nM						99%+
Nazartinib	++ mutant EGFR, Ki: 0.031 μM				++ mutant EGFR, Ki: 0.031 μM		99%+
Norcantharidin	✔						98%
CL-387785	++++ EGFR, IC50: 370 pM						98%
WHI-P154	+++ EGFR, IC50: 4 nM					VEGFR,Src	98%
Tyrphostin A9	+ EGFR, IC50: 460 μM					PDGFR	98%
AG 555	+ EGFR, IC50: 0.7 μM						99%+
AG 494	+ EGFR, IC50: 1.2 μM						99%+
AG-556	+ EGFR, IC50: 5 μM						98%
RG13022	+ EGFR, IC50: 4 μM						99%+
Tyrphostin RG 14620	✔						99%+
Vandetanib	+ EGFR, IC50: 500 nM						98%
CNX-2006	++ mutant EGFR, IC50: <20 nM				++ mutant EGFR, IC50: <20 nM		98%
AZD3759	++++ EGFR (L858R), IC50: 0.2 nM EGFR (WT), IC50: 0.3 nM						98%
Erlotinib	++++ EGFR, IC50: 2 nM						95%
Saracatinib	+++ EGFR, IC50: 5 nM EGFR (L861Q), IC50: 4 nM						99%+
AG1557	✔						98%
Rociletinib	++ EGFR (L858R/T790M), Ki: 21.5 nM EGFR (wt), Ki: 303.3 nM						98%
AG490	+ EGFR, IC50: 0.1 μM						98%
Cetuximab	++++ EGFR, Kd: 0.39 nM						99%
Osimertinib	++ L858R/T790M EGFR, IC50: 11.44 nM WT EGFR, IC50: 12.92 nM						99%
Osimertinib mesylate	✔						98% (Content MsOH 15.2-18.2%)
Chrysophanol	✔					mTOR	98%
PD153035	++++ EGFR, Ki: 5.2 pM						99%+
Olmutinib	✔					BTK	99%+
WZ4002	++++ EGFR (L858R/T790M), IC50: 8 nM EGFR (L858R), IC50: 2 nM						99%+
Icotinib	+++ EGFR, IC50: 5 nM						98+%
Desmethyl Erlotinib HCl	++++ EGFR, IC50: 2 nM						98%
Cyasterone	✔						99%+
PP 3	+ EGFR tyrosine kinase, IC50: 2.7 μM						98%
WZ8040	✔						99%+
(-)-Epigallocatechin Gallate	✔						99%
AG 18	+ EGFR, IC50: 35 μM						99%+
O-Desmethyl gefitinib	++ EGFR, IC50: 36 nM						98%
Falnidamol	✔						99%+
AZ-5104	++++ EGFR (L861Q) , IC50: <1 nM EGFR (L858R), IC50: 6 nM		+++ ErbB4, IC50: 7 nM			BRK	99%+
Butein	✔						95%
Genistein	✔						98%
SU5214	+ EGFR, IC50: 36.7 μM						99%+
Naquotinib	✔						99%+
Gefitinib	++ EGFR, IC50: 15.5 nM				+ EGFR (858R/T790M), IC50: 823.3 nM		98%
Theliatinib	+++ WT EGFR, IC50: 3 nM				++ EGFR T790M/L858R, IC50: 22 nM		98+%
Lazertinib	++++ L858R/T790M EGFR, IC50: 2 nM WT EGFR, IC50: 76 nM				++++ Del19/T790M, IC50: 1.7 nM		99%+
Gefitinib-based PROTAC 3	++ EGFR, DC50: 22.3 nM						99%+
MTX-211	✔					PI3K	99%+
(E)-AG 99	✔						99%+
Licochalcone D	✔					Caspase,PARP	97%
Zipalertinib	+++ EGFR WT, IC50: 8 nM EGFR (L861Q), IC50: 4.1 nM		+++ HER4, IC50: 4 nM		++++ EGFR L858R, IC50: 2 nM EGFR(d746-750), IC50: 1.4 nM		97%
JND3229	+++ EGFR WT, IC50: 6.8 nM				++ EGFR L858R/T790M, IC50: 30.5 nM		99%+
Firmonertinib mesylate	✔						99%+
Tyrphostin AG30	✔						99%+
EGFR-IN-12	++ EGFR, IC50: 21 nM						99%+
Mobocertinib	✔						98%
(Rac)-JBJ-04-125-02	✔						99%
(S)-Sunvozertinib	✔						98%
BLU-945	✔						95%
Poziotinib	+++ HER1, IC50: 3.2 nM		++ HER4, IC50: 23.5 nM	+++ HER2, IC50: 5.3 nM			98%
TAK-285	++ EGFR/HER1, IC50: 23 nM		+ HER4, IC50: 260 nM	++ HER2, IC50: 17 nM			99%+
ARRY-380 analog				✔			98%
Canertinib	++++ EGFR, IC50: 1.5 nM			+++ ErbB2, IC50: 9.0 nM			99%+
Dacomitinib	+++ EGFR, IC50: 6.0 nM		+ ErbB4, IC50: 73.7 nM	+ ErbB2, IC50: 45.7 nM			98%
EGFR/ErbB-2/ErbB-4 inhibitor-2			+ ErbB4, IC50: 1.91 μM	+ ErbB2, IC50: 0.08 μM			99%+
(E/Z)-CP-724714				++ HER2/ErbB2, IC50: 10 nM			98+%
Lapatinib	++ EGFR, IC50: 10.8 nM		+ ErbB4, IC50: 367 nM	+++ ErbB2, IC50: 9.2 nM			98%
AEE788	++++ EGFR, IC50: 2 nM		+ HER4/ErbB4, IC50: 160 nM	+++ HER2/ErbB2, IC50: 6 nM		c-Fms	98+%
AV-412 free base	++++ EGFR, IC50: 0.75 nM			++ ErbB2, IC50: 19 nM	++++ EGFR^L858R/T790M, IC50: 0.51 nM EGFR^T790M, IC50: 0.79 nM		98+%
Neratinib	+ EGFR, IC50: 92 nM			+ HER2, IC50: 59 nM		Src	98%
BMS-599626	++ HER1, IC50: 20 nM		+ HER4, IC50: 190 nM	++ HER2, IC50: 30 nM			99+%
Tucatinib				+++ ErbB2, IC50: 8 nM			98%
Allitinib	++++ EGFR, IC50: 0.5 nM		++++ ErbB4, IC50: 0.8 nM	+++ ErbB2, IC50: 3.0 nM			99%
Pelitinib	+ EGFR, IC50: 38.5 nM			+ ErbB2, IC50: 1.255 μM		Raf,Src	99%+
Sapitinib	+++ EGFR, IC50: 4 nM	+++ ErbB3, IC50: 4 nM		+++ ErbB2, IC50: 3 nM			99%+
CUDC-101	+++ EGFR, IC50: 2.4 nM			++ HER2, IC50: 15.7 nM		HDAC	99%+
Varlitinib	+++ ErbB1, IC50: 7 nM			++++ ErbB2, IC50: 2 nM			99%+
Afatinib dimaleate	++++ EGFR (L858R/T790M), IC50: 0.4 nM EGFR (wt), IC50: 0.5 nM			++ HER2, IC50: 14 nM			98%
Canertinib dihydrochloride	+++ EGFR, IC50: 7.4 nM			+++ ErbB2, IC50: 9 nM			98%
Allitinib tosylate	++++ EGFR, IC50: 0.5 nM EGFR (T790M/L858R), IC50: 12 nM		++++ ErbB4, IC50: 0.8 nM	+++ ErbB2, IC50: 3.0 nM			99%
Tyrphostin AG 528	+ EGFR, IC50: 4.9 μM			+ HER2, IC50: 2.1 μM			98%
Afatinib	++++ EGFR (L858R), IC50: 10 nM EGFR (wt), IC50: 0.5 nM		++++ ErbB4, IC50: 1 nM	++ HER2, IC50: 14 nM			99%
Pyrotinib dimaleate	++ EGFR, IC50: 0.013 μM			++ HER2, IC50: 0.038 μM			98+%
Epertinib HCl	++++ EGFR, IC50: 1.48 nM		+++ HER4, IC50: 2.49 nM	+++ HER2, IC50: 7.15 nM			98%
Tuxobertinib	++++ EGFR, Kd: 0.2 nM			++++ HER2, Kd: 0.76 nM			98%
ALK-IN-1					++ EGFR(C797S/del19), IC50: 138.6 nM EGFR(del19), IC50: 36.8 nM	ALK	98+%
Brigatinib					+ EGFR(C797S/T790M/del19), IC50: 67.2 nM EGFR(del19), IC50: 39.9 nM	ALK,FLT3	98%
Avitinib					++++ EGFR L858R/T790M, IC50: 0.18 nM	BTK	99%+
EAI045					✔		97%
Almonertinib					✔		98%
BI-4020					++++ EGFR^{del19 T790M C797S}, IC50: 0.2 nM		99%+
EGFR-IN-7					++++ EGFR^L858R/T790M, IC50: 0.19 nM EGFR^{d746-750/T790M/C797S}, IC50: 0.26 nM		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

AZD3759 生物活性

靶点

EGFR/ErbB1

EGFR (L858R), IC50:0.2 nM

EGFR (WT), IC50:0.3 nM
EGFR/ErbB1

EGFR (L858R), IC50:0.2 nM

EGFR (WT), IC50:0.3 nM
EGFR/ErbB1

EGFR (L858R), IC50:0.2 nM

EGFR (WT), IC50:0.3 nM

描述

Zorifertinib (AZD3759) is a highly potent, orally bioavailable EGFR inhibitor with the ability to penetrate the central nervous system. It demonstrates remarkable efficacy against EGFR mutations, exhibiting IC50 values of 0.3 nM for wild-type EGFR (EGFRwt), 0.2 nM for EGFR with the L858R mutation (EGFRL858R), and 0.2 nM for EGFR with an exon 19 deletion (EGFRexon 19Del) at ATP concentrations equivalent to Km. Zorifertinib effectively induces apoptosis in cancer cells and shows significant antitumor activity, making it a valuable candidate for research into non-small cell lung cancer (NSCLC), hepatocellular carcinoma (HCC), and potentially other malignancies^[1].At higher ATP concentrations (2 mM), the IC50 values adjust to 102 nM for EGFRwt, 7.6 nM for EGFRL858R, and 2.4 nM for EGFRexon 19Del, respectively. Furthermore, Zorifertinib inhibits phosphorylated EGFR (pEGFR) in various cell lines, including H838wt, H3255L858R, and PC-9exon 19Del, with IC50s of 64.5, 7.2, and 7.4 nM, respectively. In cellular phosphorylation assays, Zorifertinib also displays a 9-fold selectivity in inhibiting EGFR-mutant cell lines over wild-type EGFR cell lines (using the H838 cell line as a reference)^[1].

AZD3759 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
H3255 cells		Proliferation assay	72 h	Antiproliferative against human H3255 cells expressing EGFR L858R mutant after 72 hrs by MTS assay, IC50=0.007 μM	26313252
H838 cells		Function assay		Inhibition of EGFR phosphorylation in human H838 cells, IC50=0.0645 μM	26313252
PC9 cells		Function assay		Inhibition of EGFR exon19 deletion mutant phosphorylation in human PC9 cells, IC50=0.0074 μM	26313252

AZD3759 动物研究

Animal study

Pharmacokinetic studies reveal that Zorifertinib is rapidly absorbed following oral administration in rats, achieving a maximum blood concentration (Cmax) of 0.58 μM within an hour. The drug then exhibits a monoexponential decline in blood concentrations with an elimination half-life of approximately 4.3 hours, closely mirroring the half-life observed with intravenous administration (4.1 hours). Notably, the bioavailability of Zorifertinib after oral dosing in rats is reported at 91%. Similar pharmacokinetic profiles are observed in male dogs, with rapid absorption and a Cmax reached between 0.5 to 1.5 hours post-oral administration, a clearance rate of 14 mL/min per kg, a volume of distribution of 6.4 L/kg, and an elimination half-life of 6.2 hours. The oral bioavailability in dogs is excellent at 90%^[1].Zorifertinib has demonstrated significant antitumor efficacy in preclinical models, achieving 78% tumor growth inhibition at a daily dose of 7.5 mg/kg and tumor regression at 15 mg/kg daily, 4 weeks post-treatment, without causing more than 20% body weight loss. This contrasts with limited effects observed from CP-358774 in the same model. Decreases in tumor area were notably seen with Zorifertinib doses of 7.5 and 15 mg/kg. Additionally, modulation of pEGFR was confirmed through a single dose of Zorifertinib (15 mg/kg), taken 1 hour post-dosing, further evidencing the drug's target engagement^[1].

AZD3759 参考文献

[1]Zeng Q, et al. Discovery and Evaluation of Clinical 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.

AZD3759 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.17mL

0.43mL

0.22mL

10.87mL

2.17mL

1.09mL

21.74mL

4.35mL

2.17mL

AZD3759 技术信息

CAS号	1626387-80-1
分子式	C₂₂H₂₃ClFN₅O₃
分子量	459.901

别名
运输	蓝冰

存储条件

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 50 mg/mL(108.72 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验配方

AZD3759 98%

AZD3759 纯度/质量文件

全球学术期刊中引用的产品

AZD3759 生物活性

AZD3759 细胞研究

AZD3759 动物研究

AZD3759 参考文献

AZD3759 实验方案

AZD3759 技术信息

最近浏览的产品

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EGFR/ErbB1	EGFR (L858R), IC50:0.2 nM EGFR (WT), IC50:0.3 nM
EGFR/ErbB1	EGFR (L858R), IC50:0.2 nM EGFR (WT), IC50:0.3 nM
EGFR/ErbB1	EGFR (L858R), IC50:0.2 nM EGFR (WT), IC50:0.3 nM

AZD3759 98%

AZD3759 纯度/质量文件

全球学术期刊中引用的产品

AZD3759 生物活性

AZD3759 细胞研究

AZD3759 动物研究

AZD3759 参考文献

AZD3759 实验方案

AZD3759 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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