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AB141930

Erlotinib hydrochloride, EGFR tyrosine kinase inhibitor

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(6 Publications)

MW 429.9 Da, Purity >98%. Potent EGFR tyrosine kinase inhibitor (IC50 = 2 nM). Decreases EGFR autophosphorylation in tumor cells. Potent inhibitor of mutant JAK2-V617F. Weaker inhibitor of ErbB-2 kinase (Ki = 1 μM) and ErbB-4 kinase (Ki = 1.5 μM). Clinically effective agent for non-small cell lung cancer (NSCLC).

View Alternative Names

94 kDa B raf protein, Avian erythroblastic leukemia viral (v erb b) oncogene homolog, B Raf proto oncogene serine threonine protein kinase, B Raf proto oncogene, serine/threonine kinase, B raf 1, B-Raf proto-oncogene serine/threonine-protein kinase (p94), BRAF_HUMAN, C erb B2/neu protein, CD340, CD340 antigen, Cell growth inhibiting protein 40, Cell proliferation inducing protein 61, CerbB2, EGFR_HUMAN, ERBB, ERBB1, ERBB2_HUMAN, Epidermal growth factor receptor, Epidermal growth factor receptor (avian erythroblastic leukemia viral (v erb b) oncogene homolog), Epidermal growth factor receptor (erythroblastic leukemia viral (v erb b) oncogene homolog avian), Erb b2 receptor tyrosine kinase 2, ErbB-2 proto-oncogene, Errp, FLJ95109, HER 2, HER 2/NEU, HER1, Herstatin, Human epidermal growth factor receptor 2, MGC126806, MGC138284, MLN 19, Metastatic lymph node gene 19 protein, Murine sarcoma viral (v-raf) oncogene homolog B1, Murine sarcoma viral v raf oncogene homolog B1, NEU, NEU proto oncogene, NGL, NISBD2, NS7, Neuro/glioblastoma derived oncogene homolog, Neuroblastoma/glioblastoma derived oncogene homolog, Oncogen BRAF, Oncogen ERBB, PIG61, Proto-oncogene B-Raf, Proto-oncogene Neu, Proto-oncogene c-ErbB-1, Proto-oncogene c-ErbB-2, Proto-oncogene c-Rmil, RAF, RAFB 1, RMIL, Receptor tyrosine-protein kinase ErbB-1, Receptor tyrosine-protein kinase erbB-2, SA7, Serine/threonine-protein kinase B-raf, Species antigen 7, TKR1, Tyrosine kinase-type cell surface receptor HER2, Urogastrone, V erb b2 avian erythroblastic leukemia viral oncogene homolog 2, V erb b2 avian erythroblastic leukemia viral oncogene homolog 2 (neuro/glioblastoma derived oncogene homolog), V erb b2 avian erythroblastic leukemia viral oncoprotein 2, V erb b2 erythroblastic leukemia viral oncogene homolog 2, neuro/glioblastoma derived oncogene homolog, V erb b2 erythroblastic leukemia viral oncogene homolog 2, neuro/glioblastoma derived oncogene homolog (avian), Verb b2 erythroblastic leukemia viral oncogene homolog 2, neuro/glioblastoma derived-oncogene homolog, Wa5, cRmil, erb-b2 receptor tyrosine kinase 1, mENA, oncogene BRAF1, p185erbB2, p94, v raf murine sarcoma viral oncogene homolog B, v-Raf murine sarcoma viral oncogene homolog B1, v-erb-b Avian erythroblastic leukemia viral oncogen homolog, wa2

Key facts

CAS number

183319-69-9

Purity

>98%

Form

Solid

form

Molecular weight

429.9 Da

Molecular formula

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

PubChem

176871

Nature

Synthetic

Solubility

Soluble in DMSO to 25 mM (with warming)

Biochemical name

Erlotinib hydrochloride

Biological description

Potent EGFR tyrosine kinase inhibitor (IC50 = 2 nM). Decreases EGFR autophosphorylation in tumor cells. Potent inhibitor of mutant JAK2-V617F. Weaker inhibitor of ErbB-2 kinase (Ki = 1 μM) and ErbB-4 kinase (Ki = 1.5 μM). Clinically effective agent for non-small cell lung cancer (NSCLC).

Canonical smiles

COCCOC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC=CC(=C3)C#C)OCCOC.Cl

InChi

InChI=1S/C22H23N3O4.ClH/c1-4-16-6-5-7-17(12-16)25-22-18-13-20(28-10-8-26-2)21(29-11-9-27-3)14-19(18)23-15-24-22;/h1,5-7,12-15H,8-11H2,2-3H3,(H,23,24,25);1H

InChiKey

GTTBEUCJPZQMDZ-UHFFFAOYSA-N

IUPAC Name

N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine;hydrochloride

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

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

Frontiers in cell and developmental biology 10:1075364 PubMed36605723

2022

Mapping of Tilapia Lake Virus entry pathways with inhibitors reveals dependence on dynamin activity and cholesterol but not endosomal acidification.

Applications

Unspecified application

Species

Unspecified reactive species

Reem Abu Rass,Japhette Esther Kembou-Ringert,Rachel Zamostiano,Avi Eldar,Marcelo Ehrlich,Eran Bacharach

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

BMC cancer 15:957 PubMed26673416

2015

Effect of the molecular targeted drug, erlotinib, against endometrial cancer expressing high levels of epidermal growth factor receptor.

Applications

Unspecified application

Species

Unspecified reactive species

Toshio Nishimura,Kazuto Nakamura,Soichi Yamashita,Sadatomo Ikeda,Keiko Kigure,Takashi Minegishi

PloS one 10:e0120405 PubMed25793970

2015

Depsides: lichen metabolites active against hepatitis C virus.

Applications

Unspecified application

Species

Unspecified reactive species

Thi Huyen Vu,Anne-Cécile Le Lamer,Claudia Lalli,Joël Boustie,Michel Samson,Françoise Lohézic-Le Dévéhat,Jacques Le Seyec

Cell cycle (Georgetown, Tex.) 14:2171-80 PubMed25714397

2015

Combinatorial Action of MicroRNAs let-7 and miR-34 Effectively Synergizes with Erlotinib to Suppress Non-small Cell Lung Cancer Cell Proliferation.

Applications

Unspecified application

Species

Unspecified reactive species

Carlos Stahlhut,Frank J Slack
View all publications

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