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Cetuximab (anti-EGFR)

Synonyms: C225

Catalog No.A2000 Purity:99.81%

Cetuximab, a novel molecular-targeted agent,is an inhibitor of EGFR monoclonal humanized antibody interacting with the extracellular binding site of EGFR to block ligand stimulation. MW：145.781 KD.

Cetuximab (anti-EGFR) Chemical Structure

Click to purchase the isotype control of Cetuximab (anti-EGFR)

Selleck's Cetuximab (anti-EGFR) has been cited by 45 publications

Purity & Quality Control

Batch: Purity: 99.81% Protein concentration: 3.63 mg/ml Endotoxin Level: <1 EU/mg

99.81

Choose Selective EGFR Inhibitors

Name	Citation	EGFR/ErbB1	HER2/ErbB2	ErbB3	ErbB4	mutant EGFR	Others
Saracatinib (AZD0530)	279	+++					c-Src,LCK,c-YES
Canertinib (CI-1033)	46	++++	+++
AG-490	127	+					JAK2 (V617F)
CP-724714	107		++
WZ4002	34	++++
Sapitinib (AZD8931)	46	+++	+++	+++
CUDC-101	22	+++	++				HDAC,HDAC1,HDAC6
AG-1478	94	+++
PD153035 HCl	16	++++
Pelitinib (EKB-569)	11	+	+				Src,MEK/ERK,Raf
AEE788 (NVP-AEE788)	13	++++	+++		+		c-Abl,FLT1,c-Fms
AC480 (BMS-599626)	10	++	++		+
AP26113-analog (ALK-IN-1)	4					++	ALK,IGF1R,INSR
WZ3146	1	++++
Allitinib tosylate	16	++++	+++		++++
Rociletinib (CO-1686)	36	++
Varlitinib	8	+++	++++
Icotinib (BPI-2009H)	8	+++
TAK-285	4	++	++		+		MEK1,Aurora B,LCK
WHI-P154	11	+++					VEGFR,Src,JAK3
Daphnetin	4	+					PKA,PKC
PD168393	5	++++
CNX-2006	2	++				++
Tyrphostin 9	1	+					PDGFR
AG-18	1	+
4-AMino-1-phenylpyrazolo[3,4-d]pyriMidine	0	+
AST-1306	0	++++	+++		++++
ErbB2 inhibitor	0		+		+
Tuxobertinib (BDTX-189)	2	++++	++++				RIPK2,BLK
Epertinib hydrochloride	0	++++	+++		+++
JND3229	0	+++				++	EGFR C797S
BI-4020	0					++++
Tyrphostin AG-528	0	+	+
AG 556	0	+
Canertinib dihydrochloride	8	+++	+++
EGFR Inhibitor	2	++					Microtubules
SU5214	0	+					VEGFR2
RG 13022	0	+
TQB3804	0					++++
zipalertinib (TAS6417)	3	+++			+++	++++	TXK,BMX
Pyrotinib dimaleate	4	++	++
PD153035	14	++++
AG 494	0	+
AG 555	0	+
Theliatinib (HMPL-309)	0	+++				++
Avitinib (Abivertinib)	2					++++	JAK3,BTK
Lazertinib	5	++++				++++	Del19,L85R
Lifirafenib (BGB-283)	6	++				+	WT A-RAF,C-RAF (Y340/341D),BRAF(V600E)
Nazartinib (EGF816)	6	++				++
Zorifertinib (AZD3759)	6	++++
CL-387785 (EKI-785)	4	++++
Poziotinib	33	+++	+++		++
AZ5104	4	++++			+++		BLK,ACK1,BRK
AV-412 free base	0	++++	++			++++
HER2-Inhibitor-1		✔
WZ8040	✔
Genistein	✔					topo II
BDTX-1535	✔
Falnidamol	✔
BLU-945	✔
Sunvozertinib (DZD9008)	✔
CH7233163	✔
Licochalcone D	✔					PARP,Caspase,Met
Alflutinib (Furmonertinib) mesylate	✔					CYP3A4
(Rac)-JBJ-04-125-02	✔
Tyrphostin AG30 (AG30)	✔
AG-1557	✔
AG99	✔
MTX-211	✔					PI3K
RG14620	✔					ABCG2
Almonertinib (HS-10296)					✔
Cyasterone	✔
Norcantharidin	✔					c-Met
Naquotinib(ASP8273)	✔
EAI045					✔
Olmutinib (BI 1482694)	✔					BTK
Butein	✔
Chrysophanic Acid	✔					mTOR
EGCG ((-)-Epigallocatechin Gallate)		✔				FASN,DNMT,telomerase

Expand to Check More

1. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation. 2. "✔" indicates inhibitory effect, but without specific value.

Biological Activity

Description

Features

Human IgG1

Targets

EGFR ^[4]
(Cell-free assay)

0.39 nM(Kd)

In Vitro
In vitro	Cetuximab treatment increases mitochondrial priming of EGFR-expressing HeLa cells but not in EGFR-expressing MDA-MD-231 cells.^[2]
Cell Research:	Cells were lysed at a density of 1 x 10⁶/50 μL in lysis buffer (0.25 M Tris-HCl, 2% sodium dodecylsulfate, 4% β-mercaptoethanol, 10% glycerol, 0.02% bromophenol blue) supplemented with 1 X protease/phosphatase inhibitor cocktail. Cell lysates were then loaded onto polyacrylamide gels with sodium dodecyl sulfate. After electrophoresis, proteins were transferred to polyvinylidene difluoride (PVDF) membranes. The transblotted membranes were blocked for 1 hr and then probed with appropriate primary antibodies overnight at 4 ℃. Next day, the membranes were washed three times for a total of 30 min and then incubated with IRDye 680RD Donkey anti-Rabbit IgG (H + L) or IRDye 800CW Donkey anti-Mouse IgG (H + L) in darkness at room temperature for 1 h. After another three washes, scan immunoblot membranes and quantify band intensity.

In Vitro

In vitro

Cetuximab treatment increases mitochondrial priming of EGFR-expressing HeLa cells but not in EGFR-expressing MDA-MD-231 cells.^[2]

Cell Research:

Cells were lysed at a density of 1 x 10⁶/50 μL in lysis buffer (0.25 M Tris-HCl, 2% sodium dodecylsulfate, 4% β-mercaptoethanol, 10% glycerol, 0.02% bromophenol blue) supplemented with 1 X protease/phosphatase inhibitor cocktail. Cell lysates were then loaded onto polyacrylamide gels with sodium dodecyl sulfate. After electrophoresis, proteins were transferred to polyvinylidene difluoride (PVDF) membranes. The transblotted membranes were blocked for 1 hr and then probed with appropriate primary antibodies overnight at 4 ℃. Next day, the membranes were washed three times for a total of 30 min and then incubated with IRDye 680RD Donkey anti-Rabbit IgG (H + L) or IRDye 800CW Donkey anti-Mouse IgG (H + L) in darkness at room temperature for 1 h. After another three washes, scan immunoblot membranes and quantify band intensity.

In Vivo
In vivo	C225 enhanced the antitumor activity of several chemotherapeutic drugs in mouse xenograft models^[1]. Cetuximab, exerts its antitumor efficacy by multiple mechanisms that include the inhibition of cell cycle progression by arrest in the G1- phase and decreased cell number in the S-phase. Cell cycle arrest in the G1-phase also induces apoptosis by the induction and activation of proapoptotic molecules. cetuximab alone and in synergy with carboplatin resulted in decreases of tumor size, metastatic spread, and MVD in NCI-N87 tumors with EGFR cell surface expression and absence of mutations in BRAF and K-ras, whereas cetuximab had minimal in vitro effect and no in vivo treatment efficacy in tumors derived from MKN-45, in which the phenotype was also BRAF and K-ras wildtype, but which had only weak cytoplasmic EGFR protein expression^[3].
Animal Research	Objective: Antitumor activity of cetuximab in murine gastric cancer model Animal Models: Nude mouse model for human gastric cancer (CD-1/nu-nu mice) Formulation: 0.9% NaCl Dosages: 1 mg/kg Administration: i.p. Reference: https://www.ncbi.nlm.nih.gov/pubmed/22011788 Objective: To investigate the relationship between the EGFR levels and the responsiveness to cetuximab treatment in human cancer xenograft models Animal Models: Female athymic, nude mice were implanted s.c. with ~1 mm3 tumor fragments Formulation: PBS Dosages: 0.25, 0.5 or 1 mg/mouse Administration: i.p. Reference: https://www.ncbi.nlm.nih.gov/pubmed/27186886 Cetuximab can apply to nude mice, various cancer cell lines and other related assays (Only for Reference)

References
[1] Gu J, et al. Biochem Res Int. 2016, 2016:7016907. [2] Pan R, et al. Cell. 2022 Apr 28;185(9):1521-1538.e18. [3] Hotz B, et al. Gastric Cancer. 2012, 15(3):252-64.

References

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID

Product Details

CAS No.	205923-56-4
Isotype	Human IgG1
Source	CHO cells
Formulation	100 mM Pro-Ac, 20 mM Arg, pH5.0
Storage (From the date of receipt)	Store the undiluted solution at 4°C in the dark to avoid freeze-thaw cycles

Comparison of Clones for

^*Literature analysis of various clone (for this target) products available on the market shows that Selleck's selected clones are more frequently applied. (data until September 2024)

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Frequently Asked Questions

Question 1:
How to store the antibody?

Answer:
Store the undiluted solution at 4 °C in the dark. Freezing antibodies can result in a loss of activity caused by the freezing/thawing process. Diluting antibodies to working concentrations and storing at 4°C for more than a day should be avoided. Additionally, make sure to keep the antibody sterile. Under these storage conditions, your antibodies should remain active for up to one year and oftentimes longer.