Ambeed.cn

首页 / / / / AG-1478

AG-1478 {[allProObj[0].p_purity_real_show]}

货号:A103804

AG-1478选择性地抑制EGFR,IC50值为3 nM。

AG-1478 化学结构 CAS号:153436-53-4
AG-1478 化学结构
CAS号:153436-53-4
AG-1478 3D分子结构
CAS号:153436-53-4
AG-1478 化学结构 CAS号:153436-53-4
AG-1478 3D分子结构 CAS号:153436-53-4
规格 价格 会员价 库存 数量
{[ item.pr_size ]}

{[ getRatePrice(item.pr_rmb, 1,1) ]}

{[ getRatePrice(item.pr_rmb_sale, 1,1) ]} {[ suihuo_tips(item.pr_tag_price, item.pr_am) ]}

{[ getRatePrice(item.pr_rmb, 1,1) ]}

{[ getRatePrice(item.pr_rmb,item.pr_rate,1) ]} {[ suihuo_tips(item.pr_tag_price, item.pr_am) ]}
{[ getRatePrice(item.pr_rmb, 1,1) ]}{[ suihuo_tips(item.pr_tag_price, item.pr_am) ]} {[ getRatePrice(item.pr_rmb_sale, 1,1) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,item.mem_rate) ]} {[ getRatePrice(item.pr_rmb,1,item.mem_rate) ]} 现货 1周 咨询 - +
购物车0 收藏 询单

AG-1478 纯度/质量文件 产品仅供科研

货号:A103804 标准纯度: {[allProObj[0].p_purity_real_show]}
批次查询: 批次纯度:

全球学术期刊中引用的产品

Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]
Nat. Mater., 2025, 24, 1116-1125. Ambeed. [ A141030 , A131652 ]
Nat. Electron., 2025, 8, 66-74. Ambeed. [ A100095 ]
Nano-Micro Lett., 2025, 17, 311. Ambeed. [ A971305 ]
Adv. Mater., 2025, 2416621. Ambeed. [ A255324 , A420052 ]
更多 >
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 (WT), IC50: 0.3 nM

EGFR (L858R), IC50: 0.2 nM

98%
Erlotinib ++++

EGFR, IC50: 2 nM

95%
Saracatinib +++

EGFR, IC50: 5 nM

EGFR (L861Q), IC50: 4 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

99%
Osimertinib ++

L858R/T790M EGFR, IC50: 11.44 nM

WT EGFR, IC50: 12.92 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

99%
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 (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

99%
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 98%
(E)-AG 99 99%+
Licochalcone D Caspase,PARP 99%
Zipalertinib +++

EGFR (L861Q), IC50: 4.1 nM

EGFR WT, IC50: 8 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 98+%
AV-412 free base ++++

EGFR, IC50: 0.75 nM

++

ErbB2, IC50: 19 nM

++++

EGFRT790M, IC50: 0.79 nM

EGFRL858R/T790M, IC50: 0.51 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

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 2HCl +++

EGFR, IC50: 7.4 nM

+++

ErbB2, IC50: 9 nM

99%
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

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(C797S/del19), IC50: 138.6 nM

EGFR(del19), IC50: 36.8 nM

ALK 99%
Brigatinib +

EGFR(del19), IC50: 39.9 nM

EGFR(C797S/T790M/del19), IC50: 67.2 nM

ALK,FLT3 98%
Avitinib ++++

EGFR L858R/T790M, IC50: 0.18 nM

BTK 99%+
EAI045 97%
Almonertinib 99%
BI-4020 ++++

EGFRdel19 T790M C797S, IC50: 0.2 nM

99%+
EGFR-IN-7 ++++

EGFRd746-750/T790M/C797S, IC50: 0.26 nM

EGFRL858R/T790M, IC50: 0.19 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。

AG-1478 生物活性

描述 Epidermal growth factor (EGF) is a well-known growth factor that promotes cancer progression. EGF stimulates cancer growth through the EGFR receptor (EGFR) pathway. Most of cancer tissues are shown to overexpress EGFR, and EGF-EGFR axis has been considered an attractive target for cancer treatment. Indeed, EGFR-tyrosine kinase inhibitors (EGFR-TKIs) have been developed and clinically used in patients with malignancy. EGFR-TKI effectively blocks the EGFR pathway via suppression of EGFR phosphorylation and can therefore inhibit the growth of cancer cells dramaticallyIshiguro Y, Ishiguro H, Miyamoto H. Epidermal growth factor receptor tyrosine kinase inhibition up-regulates interleukin-6 in cancer cells and induces subsequent development of interstitial pneumonia. Oncotarget. 2013 Apr;4(4):550-9. doi: 10.18632/oncotarget.939. PMID: 23592411; PMCID: PMC3720603.|https://pubmed.ncbi.nlm.nih.gov/23592411/}. The quinazoline AG 1478 have been shown to selectively inhibit EGF receptor tyrosine kinase activity in vitro as compared to a variety of tyrosine kinases, including the closely related HER-2/Neu receptor. The IC50s are 0.0020 μM, 2.6 μM, > 100 μM, and >100 μM for EGFR/HER-1 HER-2/neu Insulin-R and c-src, respectively{{Osherov N, Levitzki A. Tyrphostin AG 494 blocks Cdk2 activation. FEBS Lett. 1997 Jun 30;410(2-3):187-90. doi: 10.1016/s0014-5793(97)00580-2. PMID: 9237626.|https://pubmed.ncbi.nlm.nih.gov/9237626/. In vitro study, AG1478 (1 or 10 mg/kg) was intraperitoneally injected to OVA-induced mice at 1 h before the intranasal challenge with OVA, it was showed that AG-1478 significantly and dose-dependently inhibited OVA-induced goblet cell metaplasia, mucus production and infiltration of eosinophils and neutrophils[3]. Cells were pre-treated with AG1478 antibody before EGF treatment, EGFR phosphorylation was inhibited especially in HSC-3. AG1478 also inhibited phosphorylation of STAT3, Akt, and MAPK induced by EGF. These results suggested that EGFR-TK antibody decreased cell growth via inhibiting EGF phosphorylation[4].

AG-1478 细胞研究

细胞系 浓度 检测类型 检测时间 活性说明 数据源
A431 ~10 μM Kinase assay inhibits the basal and TGF-α-stimulated tyrosine phosphorylation of the EGFR 10702262
A431 ~10 μM Function assay induces cell cycle arrest 10702262
CNE2 100 μM Growth inhibitory assay inhibits cell proliferation by 98.4% 11410322
CNE2 ~100 μM Kinase assay inhibits EGFR tyrosine phosphorylation 11410322

AG-1478 参考文献

[1]Lee FT, Mountain AJ, et al. Enhanced efficacy of radioimmunotherapy with 90Y-CHX-A''-DTPA-hu3S193 by inhibition of epidermal growth factor receptor (EGFR) signaling with EGFR tyrosine kinase inhibitor AG1478. Clin Cancer Res. 2005 Oct 1;11(19 Pt 2):7080s-7086s.

[2]Han Y, et al. Cancer Res, 1996, 56(17), 3859-3861.

[3]Shimizu S, Takezawa-Yasuoka K, Ogawa T, Tojima I, Kouzaki H, Shimizu T. The epidermal growth factor receptor inhibitor AG1478 inhibits eosinophilic inflammation in upper airways. Clin Immunol. 2018 Mar;188:1-6. doi: 10.1016/j.clim.2017.11.010. Epub 2017 Nov 26. PMID: 29183867.

[4]Ishiguro Y, Ishiguro H, Miyamoto H. Epidermal growth factor receptor tyrosine kinase inhibition up-regulates interleukin-6 in cancer cells and induces subsequent development of interstitial pneumonia. Oncotarget. 2013 Apr;4(4):550-9. doi: 10.18632/oncotarget.939. PMID: 23592411; PMCID: PMC3720603.

AG-1478 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.17mL

0.63mL

0.32mL

15.84mL

3.17mL

1.58mL

31.67mL

6.33mL

3.17mL

AG-1478 技术信息

CAS号153436-53-4
分子式C16H14ClN3O2
分子量 315.75
SMILES Code COC1=CC2=NC=NC(NC3=CC=CC(Cl)=C3)=C2C=C1OC
MDL No. MFCD00270914
别名
运输蓝冰
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, 2-8°C

溶解方案

DMSO: 50 mg/mL(158.35 mM),配合低频超声助溶,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

Ambeed 相关网站 Ambeed.cn Ambeed.com
Ambeed
关于我们
联系我们
资讯中心
网站地图
产品手册
  • 批次文件查询
  • 客户支持
    技术支持
    专业术语
    缩略词释义
    质量手册
    产品咨询
    计算器
    活动政策
    订购方法
    积分商城
    活动声明
    联系我们
    400-920-2911 sales@ambeed.cn tech@ambeed.cn
    Ambeed 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务,不为任何个人或者非科研性质用途提供服务。