AG 555 | Tyrphostin AG 555 | EGFG Inhibitor | AmBeed-信号通路专用抑制剂

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AG 555 {[allProObj[0].p_purity_real_show]}

货号：A131103 同义名： Tyrphostin AG 555;TYRPHOSTINB46

AG 555是表皮生长因子受体（EGFR）的抑制剂，IC50 为 0.7 μM。

AG 555 化学结构
CAS号：133550-34-2

AG 555 3D分子结构
CAS号：133550-34-2

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AG 555 纯度/质量文件产品仅供科研

货号：A131103 标准纯度： {[allProObj[0].p_purity_real_show]} 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: • JMC, 2024. Ambeed. [ A919389 , A918471 , A995972 ]; • Anal. Chem., 2024, 96(50): 19947-19954. Ambeed. [ A261947 , A1165388 ]; • ACS Biomater. Sci. Eng., 2024. Ambeed. [ A220462 ]; • ACS Biomater. Sci. Eng., 2024. Ambeed. [ A165235 , A110205 ]; • Pharmaceutics, 2024, 16(12): 1546. Ambeed. [ A272538 , A187261 , A691302 , A506702 ]; 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					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					VEGFR,Src	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, 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 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	✔						99%
(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			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 (wt), IC50: 0.5 nM EGFR (L858R/T790M), IC50: 0.4 nM			++ HER2, IC50: 14 nM			98%
Canertinib dihydrochloride	+++ 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(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	FLT3,ALK	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。

AG 555 生物活性

靶点

EGFR/ErbB1

EGFR, IC50:0.7 μM

描述

The epidermal growth factor receptor (EGF-R) is a tyrosine kinase transmembrane protein that is overexpressed by many epithelial malignancies, including transitional cell and renal cell carcinoma. Ligand-induced stimulation of cell growth depends on activation of the tyrosine kinase activity of the EGF-R. AG 555 is tyrphostin that have been shown to preferentially inhibit the EGF-R tyrosine kinase and thus may inhibit EGF-R-dependent cell growth^[1]. Non-cytotoxic doses of tyrphostin derivatives (AG-555, AG-18) blocked or substantially reduced Mo-MuLV replication in acute or chronically infected NIH/3T3 cellsA Esther,et al. Inhibition of Moloney murine leukemia virus replication by tyrphostins, tyrosine kinase inhibitors|FEBS Lett.1994 Mar 14;341(1):99-103.|https://pubmed.ncbi.nlm.nih.gov/8137930/. Three tyrphostins with the potency ratio AG555 >> AG18 >> AG814 were found to arrest growth with no adverse cytotoxic effects. The potency ratio to inhibit keratinocyte proliferation follows their potency to inhibit EGF receptor kinase activity in vitro^[2]. AG 555 selectively interferes with viral transcription in bovine papillomavirus type 1 (BPV-1)-transformed fibroblasts and induces suppression of cyclin-dependent kinase activity and cell cycle arrest. AG 555 treatment also led to an activation of the mitogen-activated protein kinase pathway by enhancing phosphorylation of JNK and p38. Increased JNK and p38 activity resulted in higher phosphorylation of the AP-1 family members c-Jun and activating transcription factor 2^[3]. The growth of HPV 16-immortalized human keratinocytes can be blocked by a selective EGF-R inhibitor, AG 1478, and by AG 555, a blocker of cyclin-dependent kinase 2 (Cdk2) activation. AG 1478 induces a massive increase in the Cdk2 protein inhibitors p27 and p21, whereas AG 555 inhibited the activation of Cdk2. Growth arrest induced by AG 1478 and AG 555 is accompanied by up to 20% of cells undergoing apoptosis^[4].

AG 555 临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00307866	Hepatic Neoplasms	Phase 3	Completed	-	Italy ... 展开 >> Bari, BA, Italy, 70124 Bologna, BO, Italy, 40100 Brescia, BS, Italy, 25123 Firenze, FI, Italy, 50100 Genova, GE, Italy, 16132 Milano, MI, Italy, 20132 Milano, MI, Italy, 20142 Milano, MI, Italy Palermo, PA, Italy Pisa, PI, Italy, 56126 Sassari, SS, Italy, 07100 Torino, TO, Italy, 10154 Trieste, TS, Italy, 34149 Verona, VE, Italy, 37134 Chieti, Italy, 66100 L'Aquila, Italy, 67100 Roma, Italy, 00144 Roma, Italy, 00161 Udine, Italy, 33100 收起 <<

AG 555 参考文献

[1]N Sion-Vardy,et al. Antiproliferative effects of tyrosine kinase inhibitors (tyrphostins) on human bladder and renal carcinoma cells. J Surg Res. 1995 Dec;59(6):675-80.

[2]H Ben-Bassat,et al. Tyrphostins suppress the growth of psoriatic keratinocytes. Exp Dermatol. 1995 Apr;4(2):82-8.

[3]Sabine Baars,et al. Tyrphostin AG 555 inhibits bovine papillomavirus transcription by changing the ratio between E2 transactivator/repressor function. J Biol Chem. 2003 Sep 26;278(39):37306-13.

[4]H Ben-Bassat,et al. Inhibitors of epidermal growth factor receptor kinase and of cyclin-dependent kinase 2 activation induce growth arrest, differentiation, and apoptosis of human papilloma virus 16-immortalized human keratinocytes. Cancer Res. 1997 Sep 1;57(17):3741-50.

AG 555 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

3.10mL

0.62mL

0.31mL

15.51mL

3.10mL

1.55mL

31.02mL

6.20mL

3.10mL

AG 555 技术信息

CAS号	133550-34-2
分子式	C₁₉H₁₈N₂O₃
分子量	322.358

别名	Tyrphostin AG 555;TYRPHOSTINB46
运输	蓝冰

存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Inert atmosphere,Store in freezer, under -20°C

溶解度

DMSO: 105 mg/mL(325.73 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

AG 555 {[allProObj[0].p_purity_real_show]}

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