JavaScript is disabled in your browser. Please enable JavaScript to view this website.
AB142052

Gefitinib, EGFR tyrosine kinase inhibitor

4

(1 Review)

|

(6 Publications)

MW 446.9 Da, Purity >98%. Orally active, potent, selective EGFR (Epidermal growth factor receptor) tyrosine kinase inhibitor (IC50 = 33 nM). Inhibits EGF-stimulated EGFR autophosphorylation and inhibits tumor growth in vivo. Enhances efficacy of cytotoxic agents. Inhibits growth factor production and angiogenesis. Clinically useful anticancer agent.

View Alternative Names

Alpha-PAK, B55, Beta PAK, CAM kinase II delta, CAMK 2, CAMK 2B, CAMK 2d, CAMK2G, CAMKA, CDKN1A, CaM kinase II, CaM kinase II alpha, CaM kinase II beta, CaM kinase II gamma, CaM kinase II subunit alpha, CaMK-II subunit alpha, Calcium / calmodulin dependent protein kinase II delta, Calcium/calmodulin dependent protein kinase II gamma, Calcium/calmodulin-dependent protein kinase II-alpha, Calcium/calmodulin-dependent protein kinase type II subunit alpha, Camk2a, EC 2.7.11.1, GCK family kinase MiNK, GSD9C, Gamma-PAK, Germinal center kinase like kinase, Germinal center kinase-related protein kinase, KCC2A_HUMAN, KHS, Kinase homologous to SPS1/STE20, MAP4K3, MAPK/ERK kinase kinase kinase 3, MAPK/ERK kinase kinase kinase 5, MAPK/ERK kinase kinase kinase 6, MAPKKKK3, MEK (MAP/ERK) kinase kinase 6, MEK kinase kinase 3, MEK kinase kinase 5, MEK kinase kinase 6, MEKKK 3, MEKKK 5, MEKKK6, MGC21111, MINK, MRX30, MRX47, Misshapen NIKs Related kinase, Misshapen like kinase 1, Misshapen/NIK related kinase, Mitogen activated protein kinase kinase kinase kinase 6, OPHN3, Oligophrenin 3, P21 (CDKN1A) activated kinase 2, P21 (CDKN1A) activated kinase 3, P21 protein (Cdc42/Rac) activated kinase 1, P21 protein (Cdc42/Rac) activated kinase 3, P21/Cdc42/Rac1 activated kinase 1 (yeast Ste20 related), P58, PAK alpha, PAK3beta, PAK65, PAKgamma, PHK gamma LT, PHK gamma T, PSK C3, Phosphorylase b kinase gamma catalytic chain testis/liver isoform, Phosphorylase b kinase gamma catalytic chain, liver/testis isoform, Phosphorylase kinase catalytic subunit gamma 2, Phosphorylase kinase gamma subunit 2, Phosphorylase kinase subunit gamma 2, Phosphorylase kinase, gamma 2 (testis), Phosphorylase kinase, gamma 2 (testis/liver), RAB8IPL1, RP23-122P1.6, S6/H4 kinase, STE20 homolog, yeast, Serine/threonine protein kinase PAK 2, Serine/threonine protein kinase PAK 3, Serine/threonine protein kinase PHKG2, Serine/threonine-protein kinase PAK 1, TUBA1, TUBA1A, TUBA2, TUBA3, TUBA3C, TUBA4A, Tubulin, alpha 1a, Tubulin, alpha 3c, Tubulin, alpha 4a, Ysk2, ZC3, bPAK, calcium/calmodulin-dependent protein kinase II beta, hMINK, hPAK3, mitogen-activated protein kinase kinase kinase kinase 3, p21 activated kinase 3, p21 protein (Cdc42/Rac)-activated kinase 2, p21-activated kinase 1, p21-activated kinase 2, p21/Cdc42/Rac1-activated kinase 1 (STE20 homolog, yeast), p65-PAK

1 Images
Chemical Structure - Gefitinib, EGFR tyrosine kinase inhibitor (AB142052)
  • Chemical Structure

Lab

Chemical Structure - Gefitinib, EGFR tyrosine kinase inhibitor (AB142052)

2D chemical structure image of ab142052, Gefitinib, EGFR tyrosine kinase inhibitor

Key facts

CAS number

184475-35-2

Purity

>98%

Form

Solid

form

Molecular weight

446.9 Da

Molecular formula

C<sub>2</sub><sub>2</sub>H<sub>2</sub><sub>4</sub>ClFN<sub>4</sub>O<sub>3</sub>

PubChem

123631

Nature

Synthetic

Solubility

Soluble in DMSO to 100 mM

Biochemical name

Gefitinib

Biological description

Orally active, potent, selective EGFR (Epidermal growth factor receptor) tyrosine kinase inhibitor (IC50 = 33 nM). Inhibits EGF-stimulated EGFR autophosphorylation and inhibits tumor growth in vivo. Enhances efficacy of cytotoxic agents. Inhibits growth factor production and angiogenesis. Clinically useful anticancer agent.

Canonical smiles

COC1=C(C=C2C(=C1)N=CN=C2NC3=CC(=C(C=C3)F)Cl)OCCCN4CCOCC4

InChi

InChI=1S/C22H24ClFN4O3/c1-29-20-13-19-16(12-21(20)31-8-2-5-28-6-9-30-10-7-28)22(26-14-25-19)27-15-3-4-18(24)17(23)11-15/h3-4,11-14H,2,5-10H2,1H3,(H,25,26,27)

InChiKey

XGALLCVXEZPNRQ-UHFFFAOYSA-N

IUPAC Name

N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazolin-4-amine

Properties and storage information

Shipped at conditions
Ambient - Can Ship with Ice
Appropriate short-term storage conditions
-20°C
Appropriate long-term storage conditions
-20°C
Storage information
Store under desiccating conditions

Product protocols

Publications (6)

Recent publications for all applications. Explore the full list and refine your search

Cell death discovery 10:285 PubMed38877005

2024

DUSP22 inhibits lung tumorigenesis by suppression of EGFR/c-Met signaling.

Applications

Unspecified application

Species

Unspecified reactive species

Hsiao-Han Lin,Cheng-Wei Chang,Yu-Ting Liao,Shauh-Der Yeh,Hsiu-Ping Lin,Hui-Min Ho,Chantal Hoi-Yin Cheung,Hsueh-Fen Juan,Yi-Rong Chen,Yu-Wen Su,Li-Mei Chen,Tse-Hua Tan,Wen-Jye Lin

Redox biology 69:102976 PubMed38052106

2023

Epidermal growth factor potentiates EGFR(Y992/1173)-mediated therapeutic response of triple negative breast cancer cells to cold atmospheric plasma-activated medium.

Applications

Unspecified application

Species

Unspecified reactive species

Peiyu Wang,Renwu Zhou,Rusen Zhou,Shuo Feng,Liqian Zhao,Wenshao Li,Jinyong Lin,Aleksandra Rajapakse,Chia-Hwa Lee,Frank B Furnari,Antony W Burgess,Jennifer H Gunter,Gang Liu,Kostya Ken Ostrikov,Derek J Richard,Fiona Simpson,Xiaofeng Dai,Erik W Thompson

Cancer cell 41:1480-1497.e9 PubMed37451272

2023

Tissue factor is a critical regulator of radiation therapy-induced glioblastoma remodeling.

Applications

Unspecified application

Species

Unspecified reactive species

Hye-Min Jeon,Jeong-Yub Kim,Hee Jin Cho,Won Jun Lee,Dayna Nguyen,Sung Soo Kim,Young Taek Oh,Hee-Jin Kim,Chan-Woong Jung,Gonzalo Pinero,Tanvi Joshi,Dolores Hambardzumyan,Takuya Sakaguchi,Christopher G Hubert,Thomas M McIntyre,Howard A Fine,Candece L Gladson,Bingcheng Wang,Benjamin W Purow,Jong Bae Park,Myung Jin Park,Do-Hyun Nam,Jeongwu Lee

American journal of cancer research 10:3705-3720 PubMed33294262

2020

GOLM1 upregulates expression of PD-L1 through EGFR/STAT3 pathway in hepatocellular carcinoma.

Applications

Unspecified application

Species

Unspecified reactive species

Jiuliang Yan,Binghai Zhou,Lei Guo,Zheng Chen,Bo Zhang,Shuang Liu,Wentao Zhang,Mincheng Yu,Yongfeng Xu,Yongsheng Xiao,Jian Zhou,Jia Fan,Hui Li,Qinghai Ye

Biochemistry and biophysics reports 22:100763 PubMed32322693

2020

EGF receptor inhibitors comprehensively suppress hepatitis B virus by downregulation of STAT3 phosphorylation.

Applications

Unspecified application

Species

Unspecified reactive species

Chong J Gan,Wen F Li,Chun N Li,Ling L Li,Wen Y Zhou,Xiao M Peng

Journal of clinical medicine 8: PubMed31247884

2019

Morphological State Transition Dynamics in EGF-Induced Epithelial to Mesenchymal Transition.

Applications

Unspecified application

Species

Unspecified reactive species

Vimalathithan Devaraj,Biplab Bose
View all publications

Product promise

We are committed to supporting your work with high-quality reagents, and we're here for you every step of the way. In the unlikely event that one of our products does not perform as expected, you're protected by our Product Promise.
For full details, please see our Terms & Conditions

Please note: All products are 'FOR RESEARCH USE ONLY. NOT FOR USE IN DIAGNOSTIC OR THERAPEUTIC PROCEDURES'.

For licensing inquiries, please contact partnerships@abcam.com