AZ-5104 | EGFR Inhibitor | AmBeed-信号通路专用抑制剂

AZ-5104 {[allProObj[0].p_purity_real_show]}

货号：A557620

AZ-5104是EGFR-L858R/T790M、EGFR-L858R、EGFR-L861Q和EGFR的不可逆抑制剂，IC50值分别为<1 nM、6 nM、1 nM和25 nM。AZ5104 是AZD-9291的去甲基化代谢物。

AZ-5104 化学结构
CAS号：1421373-98-9

AZ-5104 3D分子结构
CAS号：1421373-98-9

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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					PKA,PKC	95%
Lifirafenib	++ EGFR, IC50: 29 nM				+ EGFR(T790M/L858R), IC50: 495 nM		98%
PD168393	++++ EGFR, IC50: 0.70 nM						99%+
Nazartinib	++ mutant EGFR, Ki: 0.031 μM				++ mutant EGFR, Ki: 0.031 μM		98%
Norcantharidin	✔						98%
CL-387785	++++ EGFR, IC50: 370 pM						98%
WHI-P154	+++ EGFR, IC50: 4 nM					Src,VEGFR	98%
Tyrphostin A9	+ EGFR, IC50: 460 μM					PDGFR	98%
AG 555	+ EGFR, IC50: 0.7 μM						98%
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						99%
CNX-2006	++ mutant EGFR, IC50: <20 nM				++ mutant EGFR, IC50: <20 nM		99%
AZD3759	++++ EGFR (L858R), IC50: 0.2 nM EGFR (WT), IC50: 0.3 nM						98%
Erlotinib	++++ EGFR, IC50: 2 nM						95%
Saracatinib	+++ EGFR (L861Q), IC50: 4 nM EGFR, IC50: 5 nM						99%+
AG1557	✔						99%
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						95%
Osimertinib	++ WT EGFR, IC50: 12.92 nM L858R/T790M EGFR, IC50: 11.44 nM						98%
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						99%
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						99%
Falnidamol	✔						99%+
AZ-5104	++++ EGFR (L858R), IC50: 6 nM EGFR (L861Q) , IC50: <1 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		99%
Lazertinib	++++ WT EGFR, IC50: 76 nM L858R/T790M EGFR, IC50: 2 nM				++++ Del19/T790M, IC50: 1.7 nM		99%+
Gefitinib-based PROTAC 3	++ EGFR, DC50: 22.3 nM						99%+
MTX-211	✔					PI3K	98%
(E)-AG 99	✔						99%+
Licochalcone D	✔					PARP,Caspase	99%
Zipalertinib	+++ EGFR WT, IC50: 8 nM EGFR (L861Q), IC50: 4.1 nM		+++ HER4, IC50: 4 nM		++++ EGFR(d746-750), IC50: 1.4 nM EGFR L858R, IC50: 2 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	✔						95%
(S)-Sunvozertinib	✔						99%
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				✔			99%
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			95%
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/CSF1R	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			98%
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		Src,Raf	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 2HCl	+++ EGFR, IC50: 7.4 nM			+++ ErbB2, IC50: 9 nM			99%
Allitinib tosylate	++++ EGFR (T790M/L858R), IC50: 12 nM EGFR, IC50: 0.5 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			97%
Afatinib	++++ EGFR (wt), IC50: 0.5 nM EGFR (L858R), IC50: 10 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			99%
Tuxobertinib	++++ EGFR, Kd: 0.2 nM			++++ HER2, Kd: 0.76 nM			99%
ALK-IN-1					++ EGFR(del19), IC50: 36.8 nM EGFR(C797S/del19), IC50: 138.6 nM	ALK	99%
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					✔		99%
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		99%
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。

AZ-5104 生物活性

靶点

EGFR/ErbB1

EGFR (L858R), IC50:6 nM

EGFR (L861Q) , IC50:<1 nM
ErbB4

ErbB4, IC50:7 nM

描述

Epidermal growth factor receptor (EGFR) is a transmembrane protein involved in cell differentiation and proliferation upon the activation through the binding of its specific ligands. Osimertinib is a potent, irreversible inhibitor of EGFR-sensitizing and T790M-resistant mutation^[4]. AZ5104 is an active, demethylated metabolite of osimertinib, which shows the inhibition activity for EGFR (L858R/T790M), EGFR (L858R), EGFR (L861Q), and EGFR (wildtype) with IC50 values of < 1 nM, 6 nM, 1 nM and 25 nM, respectively. AZ5104 had greater potency against wild-type EGFR (33 nM in LOVO), ex19del (2 nM in PC-9), and T790M (2 nM in H1975) cell lines. AZ5104 treatment in HEK293 cells also showed more potency than osimertinib against phosphorylated HER2. In MCF10A cells stably expressing HER2^L869R/T798I, cell growth was significantly blocked after the treatment of 100 nM AZ5104 for 5 days. Treatment of 100 nM AZ5104 for 4 hours in serum-free media inhibited pAKT, pERK, and pS6 in both BT474^GFP and BT474^HER2-T798M cells^[5]. Compared to vehicle-treated mice, administration of AZ5104 (5 mg/kg/day) for one to two weeks effectively reduced the tumor volume in both C/L858R and C/L+T mice^[6].

作用机制

AZ5104 is the active metabolite of osimertinib, which targets the sensitizing and T790M resistant mutant forms of the EGFR. It binds to EGFR through targeting the cysteine-797 residue in the ATP binding site by covalent bond formation, thereby inhibiting the activity of EGFR^[6].

AZ-5104 细胞实验

Cell Line BT474 cells NR6 cells MCF10A cells H1975 PC-9 Th17 cells HepG2 cells	Concentration	Treated Time	Description	References
BT474 cells	100 nM	4 h	Test the inhibitory effect of AZ5104 on HER2T798M signaling	Cancer Discov. 2017 Jun;7(6):575-585.
NR6 cells	100 nM	4 h	Test the inhibitory effect of AZ5104 on HER2L869R/T798I signaling	Cancer Discov. 2017 Jun;7(6):575-585.
MCF10A cells	100 nM	4 h	Test the inhibitory effect of AZ5104 on HER2L869R/T798I signaling	Cancer Discov. 2017 Jun;7(6):575-585.
H1975	2 nmol/L	72 hours	Evaluate the inhibitory activity of AZ-5104 against T790M mutant cells	Transl Oncol. 2021 Feb;14(2):100961.
PC-9	2 nmol/L	72 hours	Evaluate the inhibitory activity of AZ-5104 against Del19 mutant cells	Transl Oncol. 2021 Feb;14(2):100961.
Th17 cells	above 0.5 μM	5 days	AZ5104 inhibits RORγT expression and Th17-related cytokine production in Th17 cells	Int J Mol Sci. 2019 Nov 17;20(22):5780.
HepG2 cells	1-5 μM	24 hours	AZ5104 acts as an RORγ agonist in HepG2 cells, inducing RORγ-dependent transcription and G6PC gene expression	Int J Mol Sci. 2019 Nov 17;20(22):5780.

Cell Line

BT474 cells NR6 cells MCF10A cells H1975 PC-9 Th17 cells HepG2 cells

Concentration

Treated Time

Description

References

BT474 cells

100 nM

4 h

Test the inhibitory effect of AZ5104 on HER2T798M signaling

Cancer Discov. 2017 Jun;7(6):575-585.

NR6 cells

100 nM

4 h

Test the inhibitory effect of AZ5104 on HER2L869R/T798I signaling

Cancer Discov. 2017 Jun;7(6):575-585.

MCF10A cells

100 nM

4 h

Test the inhibitory effect of AZ5104 on HER2L869R/T798I signaling

Cancer Discov. 2017 Jun;7(6):575-585.

H1975

2 nmol/L

72 hours

Evaluate the inhibitory activity of AZ-5104 against T790M mutant cells

Transl Oncol. 2021 Feb;14(2):100961.

PC-9

2 nmol/L

72 hours

Evaluate the inhibitory activity of AZ-5104 against Del19 mutant cells

Transl Oncol. 2021 Feb;14(2):100961.

Th17 cells

above 0.5 μM

5 days

AZ5104 inhibits RORγT expression and Th17-related cytokine production in Th17 cells

Int J Mol Sci. 2019 Nov 17;20(22):5780.

HepG2 cells

1-5 μM

24 hours

AZ5104 acts as an RORγ agonist in HepG2 cells, inducing RORγ-dependent transcription and G6PC gene expression

Int J Mol Sci. 2019 Nov 17;20(22):5780.

AZ-5104 动物实验

Species CB17 SCID mice Sprague-Dawley rats	Animal Model H2073-SVD and H2073-ASV xenograft model Rat plasma model	Administration	Dosage	Frequency	Description	References
CB17 SCID mice	H2073-SVD and H2073-ASV xenograft model	Oral	50 mg/kg	Once daily for 14 days	AZ5104 demonstrated significant tumor growth inhibition in H2073-SVD and H2073-ASV xenograft models	Mol Cancer Ther. 2018 May;17(5):885-896.
Sprague-Dawley rats	Rat plasma model	Plasma incubation	27 ng/ml	6 hours	Investigated the instability of AZ-5104 in rat plasma, finding its relative quantity dropped to 2.96% after 6 hours	Front Pharmacol. 2022 Jul 22;13:928983

Species

CB17 SCID mice Sprague-Dawley rats

Animal Model

H2073-SVD and H2073-ASV xenograft model Rat plasma model

Administration

Dosage

Frequency

Description

References

CB17 SCID mice

H2073-SVD and H2073-ASV xenograft model

Oral

50 mg/kg

Once daily for 14 days

AZ5104 demonstrated significant tumor growth inhibition in H2073-SVD and H2073-ASV xenograft models

Mol Cancer Ther. 2018 May;17(5):885-896.

Sprague-Dawley rats

Rat plasma model

Plasma incubation

27 ng/ml

6 hours

Investigated the instability of AZ-5104 in rat plasma, finding its relative quantity dropped to 2.96% after 6 hours

Front Pharmacol. 2022 Jul 22;13:928983

AZ-5104 动物研究

Dose

Mice: 50 mg/kg^[3] (p.o.)

Administration

p.o.

AZ-5104 参考文献

AZ-5104 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.06mL

0.41mL

0.21mL

10.30mL

2.06mL

1.03mL

20.59mL

4.12mL

2.06mL

AZ-5104 技术信息

CAS号	1421373-98-9
分子式	C₂₇H₃₁N₇O₂
分子量	485.58
SMILES Code	C=CC(NC1=CC(NC2=NC=CC(C3=CNC4=C3C=CC=C4)=N2)=C(OC)C=C1N(CCN(C)C)C)=O
MDL No.	MFCD28899992

别名
运输	蓝冰
InChI Key	IQNVEOMHJHBNHC-UHFFFAOYSA-N
Pubchem ID	71496460

存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C

溶解方案

细胞实验：

DMSO: 30 mg/mL(61.78 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：请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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

方案一

AZ-5104 {[allProObj[0].p_purity_real_show]}

AZ-5104 纯度/质量文件产品仅供科研

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AZ-5104 质控信息

AZ-5104 生物活性

AZ-5104 细胞实验

AZ-5104 动物实验

AZ-5104 动物研究

AZ-5104 参考文献

AZ-5104 实验方案

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EGFR/ErbB1	EGFR (L858R), IC50:6 nM EGFR (L861Q) , IC50:<1 nM
ErbB4	ErbB4, IC50:7 nM

AZ-5104 {[allProObj[0].p_purity_real_show]}

AZ-5104 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

AZ-5104 质控信息

AZ-5104 生物活性

AZ-5104 细胞实验

AZ-5104 动物实验

AZ-5104 动物研究

AZ-5104 参考文献

AZ-5104 实验方案

AZ-5104 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

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