Erlotinib HCl (OSI-744)

Catalog No.S1023 Synonyms: (CP358774, NSC 718781) HCl

Erlotinib HCl (OSI-744) Chemical Structure

Molecular Weight(MW): 429.90

Erlotinib HCl (OSI-744) is an EGFR inhibitor with IC50 of 2 nM in cell-free assays, >1000-fold more sensitive for EGFR than human c-Src or v-Abl.

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Cited by 83 Publications

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Biological Activity

Description Erlotinib HCl (OSI-744) is an EGFR inhibitor with IC50 of 2 nM in cell-free assays, >1000-fold more sensitive for EGFR than human c-Src or v-Abl.
Targets
HER1/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 humancolon cancer cells andMDA MB-468 human breast cancer cells. Erlotinib HCl (1 μM) induces apoptosis in DiFi humancolon 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 NVnZZ4V6TnWwY4Tpc44h[XO|YYm= M1;jXmlvcGmkaYTpc44hd2ZiRVfGVkBqdiCqdX3hckBCPDNzIHPlcIx{KGK7IFjUVmYh[XO|YYmsJGlEPTB;MD60NkDPxE1w MU[xPVgyPTRzMh?=
human SKBR3 cells NFe1UYxHfW6ldHnvckBie3OjeR?= M1nQOWlvcGmkaYTpc44hd2ZiSFXSNkBqdiCqdX3hckBUU0KUMzDj[YxteyCkeTDIWHJHKGG|c3H5MEBKSzVyPUGuPFkh|ryPLh?= Mkm4NVk5OTV2MUK=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-Met / Met / p-Axl / Axl / pERK / ERK / pEGFR / EGFR / p-STAT3 / STAT3 / p-Akt / Akt; 

PubMed: 28604685     


(b) Patient derived primary GBM neurospheres (GBM9) were exposure to erlotinib (1µM) for the indicated times followed by Western blot with the indicated antibodies. (c–d) A similar experiment in patient derived GBM neurospheres from two different patients (GBM39 and SK987). (e) U87EGFR cells were treated with erlotinib (1µM) for the indicated times followed by Western blot with the indicated antibodies. (f) Similar experiment was conducted in U87EGFRvIII cells.

p-Raf-1 / Raf-1 / p-MEK / MEK; 

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.

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.

p27 / pS10-p27 / pT157-p27 / pT187-p27; 

PubMed: 21045138     


BT-474 and SK-BR-3 cells were treated with erlotinib at 0, 1, or 3 µM for 72 h, after which expression of total p27, p27 phosphorylated at S10 (pS10-p27), pT157-p27, and pT187-p27 was assessed by western blot analysis. β-actin was used as a loading control. 

Bcl-2 / Bcl-xl / Mcl-1 / Bax / Bak / Bad / Bim EL / PUMA; 

PubMed: 17927446     


Effects of erlotinib treatment on proapoptotic and antiapoptotic proteins in H3255 cells. H3255 cells were treated with different concentrations of erlotinib for 24 h. Cell lysates were examined by immunoblotting using antibodies specific for the indicated proteins.

28604685 27508092 21045138 17927446
Immunofluorescence
Bax / Cyto C; 

PubMed: 17927446     


Erlotinib induces colocalization of BAX and cytochrome c in PC-9 cells undergoing apoptosis. Cells were grown in Lab-Tek II chambers and treated with 100 nM erlotinib or DMSO for 48 h, fixed and immunostained with antibodies against BAX (green) and cytochrome c (red) or with DAPI to detect DNA (blue). Cells were imaged by confocal microscopy.

E-cadherin / β-catenin / 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.

EGFR ; 

PubMed: 27612423     


HCC827 (delE746-A750), NCI-H3255 (L858R) and NCI-H1975 (L858R/T790M) cells were treated either with DMSO (control) or with 3 μM erlotinib/200 nM AZD9291 for the indicated time points. Cells were fixed and stained with EGFR antibody (red) and DAPI (blue, DNA dye) as described in the Materials and Methods. Representative images showing decreased EGFR immunofluorescence in erlotinib-sensitive HCC827 and NCI-H3255 cells. AZD9291 also reduced EGFR immunofluorescence even in NCI-H1975 cells. Scale bars, 10 μm. 

17927446 19825949 27612423
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. b LDH release was used to evaluate the cell death in PANC-1 cells in the presence of erlotinib. c The MTT assay for PaCa-2 cells in the presence of erlotinib treatment. d LDH release was used to evaluate the cell death in PaCa-2 cells in the presence of erlotinib.

30377412
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]
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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 colonmetric 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 with HPAC cells
  • Formulation: 6% Captisol
  • Dosages: 50 mg/kg
  • Administration: Oral administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 4 mg/mL warmed (9.3 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
15% Captisol
For best results, use promptly after mixing.
16 mg/mL warmed (suspension)

* 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 429.90
Formula

C22H23N3O4.HCl

CAS No. 183319-69-9
Storage powder
in solvent
Synonyms (CP358774, NSC 718781) HCl

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03878524 Not yet recruiting Breast Cancer|Prostate Cancer|Pancreatic Cancer|Acute Myelogenous Leukemia OHSU Knight Cancer Institute|Oregon Health and Science University|Prospect Creek Foundation March 14 2019 Phase 1
NCT03878524 Not yet recruiting Breast Cancer|Prostate Cancer|Pancreatic Cancer|Acute Myelogenous Leukemia OHSU Knight Cancer Institute|Oregon Health and Science University|Prospect Creek Foundation March 14 2019 Phase 1
NCT03720873 Recruiting EGFR Gene Mutation Fujian Cancer Hospital October 2018 Phase 2
NCT03720873 Recruiting EGFR Gene Mutation Fujian Cancer Hospital October 2018 Phase 2
NCT03653546 Recruiting Non-small Cell Lung Cancer|EGFR Gene Mutation|Brain Metastases Alpha Biopharma (Jiangsu) Co. Ltd. October 29 2018 Phase 2|Phase 3
NCT03653546 Recruiting Non-small Cell Lung Cancer|EGFR Gene Mutation|Brain Metastases Alpha Biopharma (Jiangsu) Co. Ltd. October 29 2018 Phase 2|Phase 3

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.

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Frequently Asked Questions

  • Question 1:

    Whether S1023 is suitable for mouse assays?

  • Answer:

    Dissolving S1023 in 15% Captisol is for oral gavage and it's a suspension.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID