Icotinib | BPI-2009;BPI 2009H;Conmana | EGFR | AmBeed-信号通路专用抑制剂

Icotinib/埃克替尼 {[allProObj[0].p_purity_real_show]}

货号：A120776 同义名： BPI-2009; BPI 2009H

Icotinib是一种EGFR抑制剂，IC50为5 nM，对EGFR（L858R）、EGFR（L861Q）、EGFR（T790M）和EGFR（T790M，L858R）具有抑制作用。

Icotinib/埃克替尼化学结构
CAS号：610798-31-7

Icotinib/埃克替尼 3D分子结构
CAS号：610798-31-7

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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/T790M), IC50: 14 nM EGFR (E746_A750), IC50: 2 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 (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), IC50: 2 nM EGFR (L858R/T790M), IC50: 8 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	✔					PARP,Caspase	99%
Zipalertinib	+++ EGFR (L861Q), IC50: 4.1 nM EGFR WT, IC50: 8 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	✔						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		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 (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 (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			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。

Icotinib/埃克替尼生物活性

靶点

EGFR/ErbB1

EGFR, IC50:5 nM

描述

The EGFR pathway is involved in angiogenesis, as well as cell proliferation and anti-apoptosis. EGFR encodes the EGFR (also known as ErbB1), a member of the ErbB family of receptor tyrosine kinases (RTKs). Other family members include HER2 (neu, ErbB2), HER3 (ErbB3), and HER4 (ErbB4). The ErbB RTKs are involved in intracellular signaling cascades that promote cell proliferation and survival, but can also drive malignant transformation^[1]. Icotinib is a highly-selective epidermal growth factor receptor tyrosine kinase inhibitor with an IC₅₀ of 5 nM^[2]. Icotinib can bind reversibly to ATP's binding site on EGFR protein and thus prevent completion of the signal transduction cascade^[3]. Blocking EGFRT with Icotinib treatment was sufficient to inhibit phosphorylation of Stat3 and Akt, which are key proteins in the EGFR signaling pathway, thus effectively blocking EGFR signaling pathway^[4]. A431 cells were treated with the indicated concentration of Icotinib ranging from 0 to 250 nM for 2.5 h followed 100 ng/ml of EGF for 5 min before lysis. It was demonstrated that Icotinib markedly inhibited tyrosine phosphorylation of a wide range of intracellular proteins without altering the protein level of EGFR^[2]. In a vivio study, oral administration of Icotinib at a dose of 60 mg/kg daily, five times per week significantly inhibited the volume of tumor in HCC827 xenograft models, in comparision with models^[5].

Icotinib/埃克替尼细胞实验

Cell Line PC9 and HCC827 cells H1975 PC-9/GR Human liver microsomes (HLMs) HCC4006 A549 H1781 H460 H1975 H1650 A549 HCC827 HCC827 Recombinant human UGT1A1 H460 H1299 HCC827 H1975 A549 PC-9 H1975 HCC827IR HCC827 HCC827/IcoRH HCC827/IcoRL PC9/IcoRH PC9/IcoRL HCC827IR	Concentration	Treated Time	Description	References
PC9 and HCC827 cells	10 µM	24, 48, 72 and 96 hours	Detected cell viability by MTT assay	Biomark Res. 2023 May 12;11(1):51.
H1975	2 µM	4 weeks	Assess cell viability and clonogenic capacity, H1975 was resistant to icotinib	J Exp Clin Cancer Res. 2022 Jun 11;41(1):200.
PC-9/GR	2 µM	4 weeks	Assess cell viability and clonogenic capacity, PC-9/GR was resistant to icotinib	J Exp Clin Cancer Res. 2022 Jun 11;41(1):200.
Human liver microsomes (HLMs)	0.2–60 µM	40 minutes	Evaluate the inhibitory effect of Icotinib on UGT1A1-mediated NCHN-O-glucuronidation, showing an IC50 value of 5.15 μmol/L as a noncompetitive inhibitor	Acta Pharm Sin B. 2017 Nov;7(6):657-664.
HCC4006	5 µM	48 hours	Evaluate the growth inhibitory effect of BDMC and icotinib combination on EGFR-TKI-sensitive NSCLC cells, results showed that the combination treatment had a minor effect on cell viability.	Int J Biol Sci. 2020 Mar 5;16(9):1536-1550.
A549	5 µM	48 hours	Evaluate the growth inhibitory effect of BDMC and icotinib combination on EGFR-TKI-resistant NSCLC cells, results showed that the combination treatment significantly reduced cell viability.	Int J Biol Sci. 2020 Mar 5;16(9):1536-1550.
H1781	5 µM	48 hours	Evaluate the growth inhibitory effect of BDMC and icotinib combination on EGFR-TKI-resistant NSCLC cells, results showed that the combination treatment significantly reduced cell viability.	Int J Biol Sci. 2020 Mar 5;16(9):1536-1550.
H460	5 µM	48 hours	Evaluate the growth inhibitory effect of BDMC and icotinib combination on EGFR-TKI-resistant NSCLC cells, results showed that the combination treatment significantly reduced cell viability.	Int J Biol Sci. 2020 Mar 5;16(9):1536-1550.
H1975	6.25, 12.5, 25, 50, 100 µM	48 hours	Evaluate the sensitivity of H1975 cells to Icotinib, results showed H1975 cells were resistant to Icotinib.	Int J Mol Med. 2019 Aug;44(2):437-446.
H1650	6.25, 12.5, 25, 50, 100 µM	48 hours	Evaluate the sensitivity of H1650 cells to Icotinib, results showed H1650 cells were resistant to Icotinib.	Int J Mol Med. 2019 Aug;44(2):437-446.
A549	6.25, 12.5, 25, 50, 100 µM	48 hours	Evaluate the sensitivity of A549 cells to Icotinib, results showed A549 cells were resistant to Icotinib.	Int J Mol Med. 2019 Aug;44(2):437-446.
HCC827	6.25, 12.5, 25, 50, 100 µM	48 hours	Evaluate the sensitivity of HCC827 cells to Icotinib, results showed HCC827 cells were sensitive to Icotinib.	Int J Mol Med. 2019 Aug;44(2):437-446.
HCC827	0, 2, 4, 8, 16, 32 µM	48 hours	To measure the sensitivity of HCC827 cells to Icotinib, results showed HCC827 cells were sensitive to Icotinib with IC50 of 8.1 μM.	Respir Res. 2019 Oct 12;20(1):217.
Recombinant human UGT1A1	0.2–60 µM	50 minutes	Evaluate the inhibitory effect of Icotinib on UGT1A1-mediated NCHN-O-glucuronidation, showing an IC50 value of 8.76 μmol/L as a noncompetitive inhibitor	Acta Pharm Sin B. 2017 Nov;7(6):657-664.
H460	23.60 ± 0.30 µM (IC50)	72 hours	Evaluate the growth inhibitory effect of Icotinib on H460 cells, results showed H460 cells were less sensitive to Icotinib.	J Exp Clin Cancer Res. 2019 Apr 5;38(1):148.
H1299	19.50 ± 2.86 µM (IC50)	72 hours	Evaluate the growth inhibitory effect of Icotinib on H1299 cells, results showed H1299 cells were less sensitive to Icotinib.	J Exp Clin Cancer Res. 2019 Apr 5;38(1):148.
HCC827	24.40 ± 2.88 nM (IC50)	72 hours	Evaluate the growth inhibitory effect of Icotinib on HCC827 cells, results showed HCC827 cells were sensitive to Icotinib.	J Exp Clin Cancer Res. 2019 Apr 5;38(1):148.
H1975	18.80 ± 0.40 µM (IC50)	72 hours	Evaluate the growth inhibitory effect of Icotinib on H1975 cells, results showed H1975 cells were less sensitive to Icotinib.	J Exp Clin Cancer Res. 2019 Apr 5;38(1):148.
A549	21.8 ± 0.60 µM (IC50)	72 hours	Evaluate the growth inhibitory effect of Icotinib on A549 cells, results showed A549 cells were less sensitive to Icotinib.	J Exp Clin Cancer Res. 2019 Apr 5;38(1):148.
PC-9	26.80 ± 3.62 nM (IC50)	72 hours	Evaluate the growth inhibitory effect of Icotinib on PC-9 cells, results showed PC-9 cells were sensitive to Icotinib.	J Exp Clin Cancer Res. 2019 Apr 5;38(1):148.
H1975	52.427±2.059 µM (IC50)	72 hours	Evaluate the anti-proliferative effect of Icotinib on H1975 cells, results showed H1975 cells were non-sensitive to Icotinib.	J Cancer. 2019 Jan 29;10(5):1275-1287.
HCC827IR	25.115±2.240 µM (IC50)	72 hours	Evaluate the anti-proliferative effect of Icotinib on HCC827IR cells, results showed HCC827IR cells were non-sensitive to Icotinib.	J Cancer. 2019 Jan 29;10(5):1275-1287.
HCC827	0.0126±0.0001 µM (IC50)	72 hours	Evaluate the anti-proliferative effect of Icotinib on HCC827 cells, results showed HCC827 cells were sensitive to Icotinib.	J Cancer. 2019 Jan 29;10(5):1275-1287.
HCC827/IcoRH	0.01–20 µM	96 hours	Evaluate icotinib sensitivity, results showed significantly lower sensitivity in resistant cells compared to parental cells	Biomark Res. 2021 Jan 30;9(1):9.
HCC827/IcoRL	0.01–20 µM	96 hours	Evaluate icotinib sensitivity, results showed significantly lower sensitivity in resistant cells compared to parental cells	Biomark Res. 2021 Jan 30;9(1):9.
PC9/IcoRH	0.01–20 µM	96 hours	Evaluate icotinib sensitivity, results showed significantly lower sensitivity in resistant cells compared to parental cells	Biomark Res. 2021 Jan 30;9(1):9.
PC9/IcoRL	0.01–20 µM	96 hours	Evaluate icotinib sensitivity, results showed significantly lower sensitivity in resistant cells compared to parental cells	Biomark Res. 2021 Jan 30;9(1):9.
HCC827IR	50 µM	Over 6 monthourss	To establish an Icotinib-resistant cell model, HCC827IR cells showed IC50>80 μM, indicating resistance to Icotinib.	Respir Res. 2019 Oct 12;20(1):217.

Cell Line

Concentration

Treated Time

Description

References

PC9 and HCC827 cells

10 µM

24, 48, 72 and 96 hours

Detected cell viability by MTT assay

Biomark Res. 2023 May 12;11(1):51.

H1975

2 µM

4 weeks

Assess cell viability and clonogenic capacity, H1975 was resistant to icotinib

J Exp Clin Cancer Res. 2022 Jun 11;41(1):200.

PC-9/GR

2 µM

4 weeks

Assess cell viability and clonogenic capacity, PC-9/GR was resistant to icotinib

J Exp Clin Cancer Res. 2022 Jun 11;41(1):200.

Human liver microsomes (HLMs)

0.2–60 µM

40 minutes

Evaluate the inhibitory effect of Icotinib on UGT1A1-mediated NCHN-O-glucuronidation, showing an IC50 value of 5.15 μmol/L as a noncompetitive inhibitor

Acta Pharm Sin B. 2017 Nov;7(6):657-664.

HCC4006

5 µM

48 hours

Evaluate the growth inhibitory effect of BDMC and icotinib combination on EGFR-TKI-sensitive NSCLC cells, results showed that the combination treatment had a minor effect on cell viability.

Int J Biol Sci. 2020 Mar 5;16(9):1536-1550.

A549

5 µM

48 hours

Evaluate the growth inhibitory effect of BDMC and icotinib combination on EGFR-TKI-resistant NSCLC cells, results showed that the combination treatment significantly reduced cell viability.

Int J Biol Sci. 2020 Mar 5;16(9):1536-1550.

H1781

5 µM

48 hours

Evaluate the growth inhibitory effect of BDMC and icotinib combination on EGFR-TKI-resistant NSCLC cells, results showed that the combination treatment significantly reduced cell viability.

Int J Biol Sci. 2020 Mar 5;16(9):1536-1550.

H460

5 µM

48 hours

Evaluate the growth inhibitory effect of BDMC and icotinib combination on EGFR-TKI-resistant NSCLC cells, results showed that the combination treatment significantly reduced cell viability.

Int J Biol Sci. 2020 Mar 5;16(9):1536-1550.

H1975

6.25, 12.5, 25, 50, 100 µM

48 hours

Evaluate the sensitivity of H1975 cells to Icotinib, results showed H1975 cells were resistant to Icotinib.

Int J Mol Med. 2019 Aug;44(2):437-446.

H1650

6.25, 12.5, 25, 50, 100 µM

48 hours

Evaluate the sensitivity of H1650 cells to Icotinib, results showed H1650 cells were resistant to Icotinib.

Int J Mol Med. 2019 Aug;44(2):437-446.

A549

6.25, 12.5, 25, 50, 100 µM

48 hours

Evaluate the sensitivity of A549 cells to Icotinib, results showed A549 cells were resistant to Icotinib.

Int J Mol Med. 2019 Aug;44(2):437-446.

HCC827

6.25, 12.5, 25, 50, 100 µM

48 hours

Evaluate the sensitivity of HCC827 cells to Icotinib, results showed HCC827 cells were sensitive to Icotinib.

Int J Mol Med. 2019 Aug;44(2):437-446.

HCC827

0, 2, 4, 8, 16, 32 µM

48 hours

To measure the sensitivity of HCC827 cells to Icotinib, results showed HCC827 cells were sensitive to Icotinib with IC50 of 8.1 μM.

Respir Res. 2019 Oct 12;20(1):217.

Recombinant human UGT1A1

0.2–60 µM

50 minutes

Evaluate the inhibitory effect of Icotinib on UGT1A1-mediated NCHN-O-glucuronidation, showing an IC50 value of 8.76 μmol/L as a noncompetitive inhibitor

Acta Pharm Sin B. 2017 Nov;7(6):657-664.

H460

23.60 ± 0.30 µM (IC50)

72 hours

Evaluate the growth inhibitory effect of Icotinib on H460 cells, results showed H460 cells were less sensitive to Icotinib.

J Exp Clin Cancer Res. 2019 Apr 5;38(1):148.

H1299

19.50 ± 2.86 µM (IC50)

72 hours

Evaluate the growth inhibitory effect of Icotinib on H1299 cells, results showed H1299 cells were less sensitive to Icotinib.

J Exp Clin Cancer Res. 2019 Apr 5;38(1):148.

HCC827

24.40 ± 2.88 nM (IC50)

72 hours

Evaluate the growth inhibitory effect of Icotinib on HCC827 cells, results showed HCC827 cells were sensitive to Icotinib.

J Exp Clin Cancer Res. 2019 Apr 5;38(1):148.

H1975

18.80 ± 0.40 µM (IC50)

72 hours

Evaluate the growth inhibitory effect of Icotinib on H1975 cells, results showed H1975 cells were less sensitive to Icotinib.

J Exp Clin Cancer Res. 2019 Apr 5;38(1):148.

A549

21.8 ± 0.60 µM (IC50)

72 hours

Evaluate the growth inhibitory effect of Icotinib on A549 cells, results showed A549 cells were less sensitive to Icotinib.

J Exp Clin Cancer Res. 2019 Apr 5;38(1):148.

PC-9

26.80 ± 3.62 nM (IC50)

72 hours

Evaluate the growth inhibitory effect of Icotinib on PC-9 cells, results showed PC-9 cells were sensitive to Icotinib.

J Exp Clin Cancer Res. 2019 Apr 5;38(1):148.

H1975

52.427±2.059 µM (IC50)

72 hours

Evaluate the anti-proliferative effect of Icotinib on H1975 cells, results showed H1975 cells were non-sensitive to Icotinib.

J Cancer. 2019 Jan 29;10(5):1275-1287.

HCC827IR

25.115±2.240 µM (IC50)

72 hours

Evaluate the anti-proliferative effect of Icotinib on HCC827IR cells, results showed HCC827IR cells were non-sensitive to Icotinib.

J Cancer. 2019 Jan 29;10(5):1275-1287.

HCC827

0.0126±0.0001 µM (IC50)

72 hours

Evaluate the anti-proliferative effect of Icotinib on HCC827 cells, results showed HCC827 cells were sensitive to Icotinib.

J Cancer. 2019 Jan 29;10(5):1275-1287.

HCC827/IcoRH

0.01–20 µM

96 hours

Evaluate icotinib sensitivity, results showed significantly lower sensitivity in resistant cells compared to parental cells

Biomark Res. 2021 Jan 30;9(1):9.

HCC827/IcoRL

0.01–20 µM

96 hours

Evaluate icotinib sensitivity, results showed significantly lower sensitivity in resistant cells compared to parental cells

Biomark Res. 2021 Jan 30;9(1):9.

PC9/IcoRH

0.01–20 µM

96 hours

Evaluate icotinib sensitivity, results showed significantly lower sensitivity in resistant cells compared to parental cells

Biomark Res. 2021 Jan 30;9(1):9.

PC9/IcoRL

0.01–20 µM

96 hours

Evaluate icotinib sensitivity, results showed significantly lower sensitivity in resistant cells compared to parental cells

Biomark Res. 2021 Jan 30;9(1):9.

HCC827IR

50 µM

Over 6 monthourss

To establish an Icotinib-resistant cell model, HCC827IR cells showed IC50>80 μM, indicating resistance to Icotinib.

Respir Res. 2019 Oct 12;20(1):217.

Icotinib/埃克替尼动物实验

Species BALBL/c nude mice Nude mice Nude mice BALB/c nude mice BALB/c nude mice	Animal Model H460 cell xenograft model Subcutaneous xenograft model Subcutaneous xenograft model HCC827IR and H1975 xenograft models PC-9 xenograft model	Administration	Dosage	Frequency	Description	References
BALBL/c nude mice	H460 cell xenograft model	Oral gavage	125 mg/kg icotinib and 100 mg/kg BDMC	Once daily for 21 days	Evaluate the anti-tumor effect of BDMC and icotinib combination on H460 cell xenograft model, results showed that the combination treatment significantly inhibited tumor growth.	Int J Biol Sci. 2020 Mar 5;16(9):1536-1550.
Nude mice	Subcutaneous xenograft model	Oral	50 mg/kg	21 days	Evaluate the anti-tumor effect of Icotinib in vivo, found that STAT3/FOXM1 signaling blockade reversed resistance	J Exp Clin Cancer Res. 2022 Jun 11;41(1):200.
Nude mice	Subcutaneous xenograft model	Oral	50 mg/kg	Every three days for three weeks	Evaluate the antitumor effect of icotinib in vivo, results showed lower sensitivity to icotinib in tumors formed by resistant cells	Biomark Res. 2021 Jan 30;9(1):9.
BALB/c nude mice	HCC827IR and H1975 xenograft models	Oral	50 mg/kg	Thrice weekly for 5 weeks	Evaluate the anti-tumor effect of Icotinib on HCC827IR and H1975 xenograft models, results showed Icotinib alone had limited effect on HCC827IR model and no significant effect on H1975 model.	J Cancer. 2019 Jan 29;10(5):1275-1287.
BALB/c nude mice	PC-9 xenograft model	Intratumoral injection	60 mg/kg	17 days	Evaluate the antitumor effect of Icotinib on PC-9 xenograft model in vivo, results showed Icotinib significantly inhibited tumor growth.	J Exp Clin Cancer Res. 2019 Apr 5;38(1):148.

Species

BALBL/c nude mice Nude mice Nude mice BALB/c nude mice BALB/c nude mice

Animal Model

H460 cell xenograft model Subcutaneous xenograft model Subcutaneous xenograft model HCC827IR and H1975 xenograft models PC-9 xenograft model

Administration

Dosage

Frequency

Description

References

BALBL/c nude mice

H460 cell xenograft model

Oral gavage

125 mg/kg icotinib and 100 mg/kg BDMC

Once daily for 21 days

Evaluate the anti-tumor effect of BDMC and icotinib combination on H460 cell xenograft model, results showed that the combination treatment significantly inhibited tumor growth.

Int J Biol Sci. 2020 Mar 5;16(9):1536-1550.

Nude mice

Subcutaneous xenograft model

Oral

50 mg/kg

21 days

Evaluate the anti-tumor effect of Icotinib in vivo, found that STAT3/FOXM1 signaling blockade reversed resistance

J Exp Clin Cancer Res. 2022 Jun 11;41(1):200.

Nude mice

Subcutaneous xenograft model

Oral

50 mg/kg

Every three days for three weeks

Evaluate the antitumor effect of icotinib in vivo, results showed lower sensitivity to icotinib in tumors formed by resistant cells

Biomark Res. 2021 Jan 30;9(1):9.

BALB/c nude mice

HCC827IR and H1975 xenograft models

Oral

50 mg/kg

Thrice weekly for 5 weeks

Evaluate the anti-tumor effect of Icotinib on HCC827IR and H1975 xenograft models, results showed Icotinib alone had limited effect on HCC827IR model and no significant effect on H1975 model.

J Cancer. 2019 Jan 29;10(5):1275-1287.

BALB/c nude mice

PC-9 xenograft model

Intratumoral injection

60 mg/kg

17 days

Evaluate the antitumor effect of Icotinib on PC-9 xenograft model in vivo, results showed Icotinib significantly inhibited tumor growth.

J Exp Clin Cancer Res. 2019 Apr 5;38(1):148.

Icotinib/埃克替尼参考文献

Icotinib/埃克替尼实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.55mL

0.51mL

0.26mL

12.77mL

2.55mL

1.28mL

25.55mL

5.11mL

2.55mL

Icotinib/埃克替尼技术信息

CAS号	610798-31-7
分子式	C₂₂H₂₁N₃O₄
分子量	391.42
SMILES Code	C#CC1=CC(NC2=C3C=C(OCCOCCOCCO4)C4=CC3=NC=N2)=CC=C1
MDL No.	MFCD22124501

别名	BPI-2009; BPI 2009H; Conmana
运输	蓝冰
InChI Key	QQLKULDARVNMAL-UHFFFAOYSA-N
Pubchem ID	22024915

存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, sealed in dry, 2-8°C

溶解方案

细胞实验：

DMSO: 150 mg/mL(383.22 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

方案二

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Icotinib/埃克替尼动物实验

Icotinib/埃克替尼参考文献

Icotinib/埃克替尼实验方案

Icotinib/埃克替尼技术信息

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Icotinib/埃克替尼 {[allProObj[0].p_purity_real_show]}

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全球学术期刊中引用的产品

Icotinib/埃克替尼 质控信息

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Icotinib/埃克替尼 细胞实验

Icotinib/埃克替尼 动物实验

Icotinib/埃克替尼 参考文献

Icotinib/埃克替尼 实验方案

Icotinib/埃克替尼 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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热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

Icotinib/埃克替尼纯度/质量文件产品仅供科研

Icotinib/埃克替尼质控信息

Icotinib/埃克替尼生物活性

Icotinib/埃克替尼细胞实验

Icotinib/埃克替尼动物实验

Icotinib/埃克替尼参考文献

Icotinib/埃克替尼实验方案

Icotinib/埃克替尼技术信息