Erlotinib

Catalog No.S7786 Synonyms: CP358774, NSC 718781

Erlotinib Chemical Structure

Molecular Weight(MW): 393.44

Erlotinib is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl.

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Cited by 150 Publications

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Biological Activity

Description Erlotinib is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl.
Targets
EGFR [1]
(Cell-free assay)
2 nM
In vitro

Erlotinib HCl potently inhibits EGFR activation in intact cells including HNS human head and neck tumor cells (IC50 20nM), DiFi human colon cancer cells and MDA MB-468 human breast cancer cells. Erlotinib HCl (1 μM) induces apoptosis in DiFi human colon cancer cells. [1] Erlotinib inhibits growth of a panel of NSCLC cell lines including A549, H322, H3255, H358 H661, H1650, H1975, H1299, H596 with IC50 ranging from 29 nM to >20 μM. [2] Erlotinib HCl(2 μM) significantly inhibits growth of AsPC-1 and BxPC-3 pancreatic cells. [3] The effects of Erlotinib HCl in combination with gemcitabine are considered additive in KRAS-mutated pancreatic cancer cells. Ten micromolar of Erlotinib HCl inhibits EGFR phospho-rylation at the Y845 (Src-dependent phosphorylation) and Y1068 (auto-phosphorylation) sites. [4] Combination with Erlotinib HCl could down-modulate rapamycin-stimulated Akt activity and produces a synergistic effect on cell growth inhibition. [5]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human A431 cells M3u2fWZ2dmO2aX;uJIF{e2G7 NEXrWGhKdmirYnn0bY9vKG:oIFXHSnIhcW5iaIXtZY4hSTR|MTDj[YxteyCkeTDIWHJHKGG|c3H5MEBKSzVyPUCuOFIh|ryPLh?= MWmxPVgyPTRzMh?=
human SKBR3 cells NEXnSFFHfW6ldHnvckBie3OjeR?= MkPjTY5pcWKrdHnvckBw\iCKRWKyJIlvKGi3bXHuJHNMSlJ|IHPlcIx{KGK7IFjUVmYh[XO|YYmsJGlEPTB;MT64PUDPxE1w NF35PG8yQThzNUSxNi=>

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
Cleaved PARP / PARP ; 

PubMed: 27508092     


HCC827 or H1650 cells were treated with DMSO, celecoxib, erlotinib alone, or in combination for 48 h. Western blot analysis showed that cleaved PARP was higher in cells after combination treatment.

P-Raf-1 / t-Raf-1 / p-MEK / t-MEK / p-ERK / t-ERK / p-PI3K / t-PI3K / p-AKT / AKT; 

PubMed: 27508092     


Cells from both ER and ECR groups were treated with 3 μM erlotinib for 72 h. Cell lysates were used for Western blotting with indicated antibodies.

p-STAT3 / STAT3 / PTPMeg2 / p-EGFR / EGFR / pJAK2 / JAK2 / Bcl2 / Bcl-xl / Survivin; 

PubMed: 24019973     


Tu212 and Tu686 cells were treated with erlotinib (0.1µM) for various times. Levels of various proteins (pSTAT3, PTPMeg2, pEGFR, Bcl2, Bcl-XL, etc.) were analyzed by Western blot. 

27508092 24019973
Immunofluorescence
β-catenin; 

PubMed: 25209444     


Distribution of β-catenin by immunofluorescence staining after erlotinib treatment for 48h. These experiments were repeated in triplicate.

E-cadherin / Vimentin ; 

PubMed: 19825949     


SUM149 cells were plated in 3D culture without or with erlotinib for 4 days. Immunofluorescence analysis was performed to detect E-cadherin, β-catenin, and vimentin. Nuclei were visualized with DAPI. D, SUM149 cells were transfected with control or ERK si䲧疝Ỵ疞㧀疜膉痘 瘿�෋ᾰƌ෋à 㺣痖帉痖Ѐ瑖堘𢡄빢᎒෋à鑸᎒彿堙奋堙巫堙᎒ﻺ᎒彿堙ﻮ᎒塚堙ﻺ᎒ꍈ堞빢᎒學堙漸堞圔堙빢᎒圞堙圭堙𢡄玚Wᾰƌ

25209444 19825949
Growth inhibition assay
Cell viability ; 

PubMed: 30377412     


a The MTT assay for PANC-1 viability. Different doses of erlotinib were added to the medium of PANC-1 cells. c The MTT assay for PaCa-2 cells in the presence of erlotinib treatment. 

IC50; 

PubMed: 17671085     


dose-response curves of A-431 cells and 10 breast cancer cell lines after treatment with erlotinib at final concentrations of 0.03, 0.06, 0.1, 0.2, 0.3, 0.6, 1, 2, 3, 6, 10, or 20 μmol/L for 72 h. The surviving fractions were determined by MTT assay. Poin䲧疝Ỵ疞㧀疜膉痘 瘿�෋ᾰƌ෋à 㺣痖帉痖Ѐ

30377412 17671085
In vivo At doses of 100 mg/kg, Erlotinib HCl completely prevents EGF-induced autophosphorylation of EGFR in human HN5 tumors growing as xenografts in athymic mice and of the hepatic EGFR of the treated mice. [1] Erlotinib HCl (100 mg/Kg) inhibits H460a and A549 tumor models with 71 and 93% inhibition rate. [5]

Protocol

Kinase Assay:

[1]
+ Expand

Kinase assays:

96-well plates are coated by incubation overnight at 37 °C with 100 μL per well of 0.25 mg/mL PGT in PBS. Excess PGT is removed by aspiration, and the plate is washed 3 times with washing buffer (0.1% Tween 20 in PBS). The kinase reaction is performed in 50 μL of 50 mM HEPES (pH 7.3), containing 125 mM sodium chloride, 24 mM magnesium chloride, 0.1 mM sodium orthovanadate, 20 μM ATP, 1.6 μg/mL EGF, and 15 ng of EGFR, affinity purified from A431 cell membranes. Erlotinib HCl in DMSO is added to give a final DMSO concentration of 2.5%. Phosphorylation is initiated by addition of ATP and proceeded for 8 minutes at room temperature, with constant shaking. The kinase reaction is terminated by aspiration of the reaction mixture and is washed 4 times with washing buffer. Phosphorylated PGT is measured by 25 minutes of incubation with 50 μL per well HRP-conjugated PY54 antiphosphotyrosine antibody, diluted to 0.2 μg/mL in blocking buffer (3% BSA and 0.05% Tween 20 in PBS). Antibody is removed by aspiration, and the plate is washed 4 times with washing buffer. The colorimetric signal is developed by addition of TMB Microwell Peroxidase Substrate, 50μL per well, and stopped by the addition of 0.09 M sulfuric acid, 50 μL per well. Phosphotyrosine is estimated by measurement of absorbance at 450 nm. The signal for controls is typically 0.6-1.2 absorbance units, with essentially no back ground in wells without AlP, EGFR, or PGT and is proportional to the time of incubation for 10 minutes.
Cell Research:

[2]
+ Expand
  • Cell lines: A549, H322, H3255, H358 H661, H1650, H1975, H1299, H596 cells
  • Concentrations: 30 nM-20 μM
  • Incubation Time: 72 hours
  • Method:

    Exponentially growing cells are seeded in 96-well plastic plates and exposed to serial dilutions of erlotinib, pemetrexed, or the combination at a constant concentration ratio of 4:1 in triplicates for 72 h. Cell viability is assayed by cell count and the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. Growth inhibition is expressed as the percentage of surviving cells in drug-treated versus PBS-treated control cells (which is considered as 100% viability). The IC50 value is the concentration resulting in 50% cell growth inhibition by a 72-h exposure to drug(s) compared with untreated control cells and is calculated by the CalcuSyn software.


    (Only for Reference)
Animal Research:

[6]
+ Expand
  • Animal Models: Male 5-week-old BALB-nu/nu mice with HPAC cells
  • Formulation: 6% Captisol
  • Dosages: 50 mg/kg
  • Administration: Oral administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 78 mg/mL (198.25 mM)
Ethanol 15 mg/mL warmed (38.12 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing. 		6mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 393.44
Formula

C22H23N3O4
CAS No. 183321-74-6
Storage powder
in solvent
Synonyms CP358774, NSC 718781

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03460678 Recruiting Drug: Pemetrexed|Drug: Erlotinib Carcinoma Non-Small-Cell Lung Hikma Pharmaceuticals LLC February 28 2018 Phase 4
NCT02942095 Active not recruiting Drug: Ixazomib|Drug: Erlotinib Solid Tumors M.D. Anderson Cancer Center|Millennium: The Takeda Oncology Company March 6 2017 Phase 1
NCT02991651 Recruiting Drug: IRX4204|Drug: erlotinib Lung Cancer Nonsmall Cell Io Therapeutics|Dartmouth College May 2016 Phase 1
NCT02495233 Terminated Drug: Gilteritinib|Drug: Erlotinib Non-Small-Cell Lung Cancer Astellas Pharma Global Development Inc.|Astellas Pharma Inc September 8 2015 Phase 1|Phase 2
NCT02468661 Terminated Drug: INC280 single agent|Drug: Erlotinib Non-Small Cell Lung Cancer Novartis Pharmaceuticals|Novartis September 23 2015 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

  • Question 1:

    Can you please give me some advice for which solvent we should use to dissolve it for animal studies?

  • Answer:

    For in vivo application, we recommend to use 5% DMSO+45% PEG 300+ddH2O up to 6mg/ml.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID