PD153035 | AG1517 | EGFR Inhibitor | AmBeed-信号通路专用抑制剂

PD153035 {[allProObj[0].p_purity_real_show]}

货号：A100205 同义名： AG1517; ZM 252868

PD153035 是一种 EGFR 酪氨酸激酶抑制剂，IC50 值为 25 nM。PD153035 具有抗肿瘤作用，可用于研究 EGFR 相关的信号通路和癌症治疗。

PD153035 化学结构
CAS号：153436-54-5

PD153035 3D分子结构
CAS号：153436-54-5

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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					PKC,PKA	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 (L861Q), IC50: 4 nM EGFR, IC50: 5 nM						99%+
AG1557	✔						99%
Rociletinib	++ EGFR (wt), Ki: 303.3 nM EGFR (L858R/T790M), Ki: 21.5 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 (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	++++ 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	✔					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/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 (wt), IC50: 0.5 nM EGFR (L858R/T790M), IC50: 0.4 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(C797S/del19), IC50: 138.6 nM EGFR(del19), IC50: 36.8 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。

PD153035 生物活性

靶点

EGFR/ErbB1

EGFR, Ki:5.2 pM

描述

Many of the tyrosine kinase enzymes which are early components of the growth signal transduction pathway in mammalian cells are encoded by proto-oncogenes, and their transformation or overexpression has been shown to occur in a large percentage of clinical cancers. The epidermal growth factor receptor (EGFR), one of the tyrosine kinase enzymes, has thus become important target for cancer therapy. PD153035 is a potent and selective inhibitor against EGFR with an IC₅₀ value of 25 pM and K_i value of 6 pM. PD153035 inhibited EGF-stimulated receptor autophosphorylation in A431 human epidermoid carcinoma cells, with IC₅₀ of 14 nM ^[3]. In cell lines with the highest level of EGFR overexpression, PD153035 concentrations of ≥ 75 nM resulted in complete inhibition of receptor autophosphorylation. PD153035 caused a dose-dependent growth inhibition of EGFR-positive cell lines, beginning at less than micromolar concentrations, and the IC₅₀ was less than 1 μM in most cases ^[4].

作用机制

PD153035 binds at the ATP site of EGFR .

PD153035 细胞实验

Cell Line DU-145 cells PC-3 cells SKOV3 cells CaOV3 cells A549 cells BeWo cells BeWo cells Normal human epidermal keratinocytes (NHEKs) AGS gastric epithelial cells HCT116 colon cancer cells	Concentration	Treated Time	Description	References
DU-145 cells	500 nM	72 hours	Reversed EGF-induced decrease in miR-200c expression	Cancer Lett. 2018 Sep 1;431:1-10.
PC-3 cells	500 nM	72 hours	Reversed EGF-induced decrease in miR-200c expression	Cancer Lett. 2018 Sep 1;431:1-10.
SKOV3 cells	1 µM	1 hour	PD153035 and AG1478 blocked EGF-induced EGFR activation (phosphorylation at Tyr 1068), but had no effect on EGF-induced EGFR down-regulation.	Cancer Lett. 2008 Aug 8;266(2):249-62.
CaOV3 cells	1 µM	1 hour	PD153035 inhibits EGF-induced EGFR, and downstream AKT/ERK activation, but cannot reverse EGF-induced EGFR down-regulation.	Cancer Lett. 2008 Aug 8;266(2):249-62.
A549 cells	1 µM	1 hour	To investigate the inhibitory effect of PD153035 on the EGF signaling pathway and its impact on mitochondrial dynamics. Results showed that PD153035 inhibits the EGF signaling pathway and promotes mitochondrial fusion.	Cells. 2022 Feb 11;11(4):624.
BeWo cells	0-1 µM	24 hours	PD153035 inhibited EGFR phosphorylation and reduced Ki67 expression, indicating that EGFR is activated without exogenous stimulation.	Cell Mol Life Sci. 2012 Dec;69(23):4029-40.
BeWo cells	0-1 µM	24 hours	PD153035 inhibited EGFR phosphorylation and partially reversed the enhanced proliferation observed following SHP-1 knockdown	Cell Mol Life Sci. 2012 Dec;69(23):4029-40.
Normal human epidermal keratinocytes (NHEKs)	300 or 600 nM	24 hours	PD153035 significantly inhibited scratch-induced CCL20 upregulation and decreased baseline CCL20 production in non-scratched controls	Int J Mol Sci. 2020 Jan 9;21(2):434.
AGS gastric epithelial cells	5 µM	30 min pretreatment followed by H. pylori infection for 4 hours	Inhibited H. pylori-mediated Egr-1 upregulation, demonstrating EGFR transactivation plays a role in this process	Gut. 2005 Oct;54(10):1363-9.
HCT116 colon cancer cells	0-20 µM	72 hours	To evaluate the effect of PD153035 on proliferation and apoptosis of colon cancer stem cells. Results showed that PD153035 inhibited tumorosphere formation in a dose-dependent manner.	Cell Prolif. 2012 Oct;45(5):413-9.

Cell Line

Concentration

Treated Time

Description

References

DU-145 cells

500 nM

72 hours

Reversed EGF-induced decrease in miR-200c expression

Cancer Lett. 2018 Sep 1;431:1-10.

PC-3 cells

500 nM

72 hours

Reversed EGF-induced decrease in miR-200c expression

Cancer Lett. 2018 Sep 1;431:1-10.

SKOV3 cells

1 µM

1 hour

PD153035 and AG1478 blocked EGF-induced EGFR activation (phosphorylation at Tyr 1068), but had no effect on EGF-induced EGFR down-regulation.

Cancer Lett. 2008 Aug 8;266(2):249-62.

CaOV3 cells

1 µM

1 hour

PD153035 inhibits EGF-induced EGFR, and downstream AKT/ERK activation, but cannot reverse EGF-induced EGFR down-regulation.

Cancer Lett. 2008 Aug 8;266(2):249-62.

A549 cells

1 µM

1 hour

To investigate the inhibitory effect of PD153035 on the EGF signaling pathway and its impact on mitochondrial dynamics. Results showed that PD153035 inhibits the EGF signaling pathway and promotes mitochondrial fusion.

Cells. 2022 Feb 11;11(4):624.

BeWo cells

0-1 µM

24 hours

PD153035 inhibited EGFR phosphorylation and reduced Ki67 expression, indicating that EGFR is activated without exogenous stimulation.

Cell Mol Life Sci. 2012 Dec;69(23):4029-40.

BeWo cells

0-1 µM

24 hours

PD153035 inhibited EGFR phosphorylation and partially reversed the enhanced proliferation observed following SHP-1 knockdown

Cell Mol Life Sci. 2012 Dec;69(23):4029-40.

Normal human epidermal keratinocytes (NHEKs)

300 or 600 nM

24 hours

PD153035 significantly inhibited scratch-induced CCL20 upregulation and decreased baseline CCL20 production in non-scratched controls

Int J Mol Sci. 2020 Jan 9;21(2):434.

AGS gastric epithelial cells

5 µM

30 min pretreatment followed by H. pylori infection for 4 hours

Inhibited H. pylori-mediated Egr-1 upregulation, demonstrating EGFR transactivation plays a role in this process

Gut. 2005 Oct;54(10):1363-9.

HCT116 colon cancer cells

0-20 µM

72 hours

To evaluate the effect of PD153035 on proliferation and apoptosis of colon cancer stem cells. Results showed that PD153035 inhibited tumorosphere formation in a dose-dependent manner.

Cell Prolif. 2012 Oct;45(5):413-9.

PD153035 动物实验

Species Rats Mice	Animal Model Schizophrenia animal model Partial liver transplantation model	Administration	Dosage	Frequency	Description	References
Rats	Schizophrenia animal model	Intraventricular infusion	1.0, 0.1 or 0.01 mg/ml	14 days	PD153035 ameliorated the deficits in startle response and prepulse inhibition in a dose-dependent manner and reduced the bursting activity of nigral dopamine neurons.	Transl Psychiatry. 2013 Apr 30;3(4):e252
Mice	Partial liver transplantation model	Intraperitoneal injection	30 mg/kg	Injected immediately after transplantation	PD153035 inhibited EGFR activity, significantly reducing BrdU labeling and mitotic index in 50%-size liver grafts and largely abrogated the stimulation of regeneration by AR in 30%-size liver grafts.	Am J Transplant. 2012 Aug;12(8):2052-61

Species

Rats Mice

Animal Model

Schizophrenia animal model Partial liver transplantation model

Administration

Dosage

Frequency

Description

References

Rats

Schizophrenia animal model

Intraventricular infusion

1.0, 0.1 or 0.01 mg/ml

14 days

PD153035 ameliorated the deficits in startle response and prepulse inhibition in a dose-dependent manner and reduced the bursting activity of nigral dopamine neurons.

Transl Psychiatry. 2013 Apr 30;3(4):e252

Mice

Partial liver transplantation model

Intraperitoneal injection

30 mg/kg

Injected immediately after transplantation

PD153035 inhibited EGFR activity, significantly reducing BrdU labeling and mitotic index in 50%-size liver grafts and largely abrogated the stimulation of regeneration by AR in 30%-size liver grafts.

Am J Transplant. 2012 Aug;12(8):2052-61

PD153035 参考文献

PD153035 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.78mL

0.56mL

0.28mL

13.88mL

2.78mL

1.39mL

27.76mL

5.55mL

2.78mL

PD153035 技术信息

CAS号	153436-54-5
分子式	C₁₆H₁₄BrN₃O₂
分子量	360.21
SMILES Code	COC1=CC2=NC=NC(NC3=CC=CC(Br)=C3)=C2C=C1OC
MDL No.	MFCD00934896

别名	AG1517; ZM 252868; NSC 669364; SU-5271
运输	蓝冰
InChI Key	LSPANGZZENHZNJ-UHFFFAOYSA-N
Pubchem ID	4705

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

细胞实验：

DMSO: 35 mg/mL(97.17 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

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

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