Erlotinib (OSI-774) HCl

Catalog No.S1023 Synonyms: CP358774, NSC 718781,OSI-774 HCl

For research use only.

Erlotinib (OSI-774, CP358774, NSC 718781) HCl 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.

Erlotinib (OSI-774) HCl Chemical Structure

CAS No. 183319-69-9

Selleck's Erlotinib (OSI-774) HCl has been cited by 509 publications

Purity & Quality Control

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Biological Activity

Description Erlotinib (OSI-774, CP358774, NSC 718781) HCl 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 SKBR3 cells NUHaU4xOTnWwY4Tpc44h[XO|YYm= NFXnfJZKdmirYnn0bY9vKG:oIFjFVlIhcW5iaIXtZY4hW0uEUkOgZ4VtdHNiYomgTHRTTiCjc4PhfUwhUUN3ME2xMlg6KM7:TT6= M1PldVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OEG1OFEzLz5zOUixOVQyOjxxYU6=
human A431 cells MWnGeY5kfGmxbjDhd5NigQ>? NIPBXFZKdmirYnn0bY9vKG:oIFXHSnIhcW5iaIXtZY4hSTR|MTDj[YxteyCkeTDIWHJHKGG|c3H5MEBKSzVyPUCuOFIh|ryPLh?= MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQThzNUSxNkc,OTl6MUW0NVI9N2F-
A431 NGfNNJhHfW6ldHnvckBie3OjeR?= MV\Jcohq[mm2aX;uJI9nKEWJRmKgbY4hcHWvYX6gRVQ{OSClZXzsd{BjgSCyaH;zdIhwfHm{b4PpcoUhTUyLU1GgZZN{[XluIFnDOVAhRSByLkCwNVIh|ryPLh?= MnPGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR6OUC2OVIoRjJ2OEmwOlUzRC:jPh?=
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MCF7 NFXiVHpCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MlvINVIhcHK| NFrLPIhCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3DSlch[2WubIOgZYZ1\XJiMUKgbJJ{KGK7IF3UWEBie3OjeTygTWM2OCB;IECuNUDPxE1w NUH5XZVWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[2OVI1QDJpPkK2OlUzPDh{PD;hQi=>
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HepG2 MUHBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MkLDOFghcHK| Mny2RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKZYDHNkBk\WyuczDh[pRmeiB2ODDodpMh[nliTWTUJIF{e2G7LDDJR|UxKD1iMD6xNkDPxE1w NXPjUXpQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2N|A1OTJpPkK0OlMxPDF{PD;hQi=>
HepG2 MX;DfZRwfG:6aXPpeJkh[XO|YYm= MmrLOFghcHK| NUH2R4g4S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUGWyR{KgZ4VtdHNiYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygTWM2OCB;IECuNVIh|ryPLh?= M1f0O|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MUS0PFU1Lz5{NEG0OFg2PDxxYU6=
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U251 Mni3SpVv[3Srb36gZZN{[Xl? NH\SW|A3OCCvaX7z MlvPTY5pcWKrdHnvckBw\iCYRVfGVlIhcW5iaIXtZY4hXTJ3MTDj[YxteyClb33wc5Vv\CCycnX0doVifGWmIH\vdkA3OCCvaX6gZoVnd3KnIG\FS2Yhe3SrbYXsZZRqd25iZn;yJFExKG2rboOgZpkheGixc4Doc5R6em:|aX7lJGVNUVODIHP5eI9jdG:2IH3leIhw\CxiSVO1NEA:KDBwMUK0O{DPxE1w M3vX[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OEiyOVE6Lz5{NUi4NlUyQTxxYU6=
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MLMA NYPvOY9pT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{jDTWlEPTBiPTCzPE43PTJizszN M{O2bVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU2Oy9pPmPBUmdGWjxxYU6=
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LP-1 NIf1eWFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3rMVWlEPTBiPTCzPU41PDF3IN88US=> MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1OVMwLz6VQV7HSXI9N2F-
ONS-76 MorOS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NIPKOmpKSzVyIE2gN|kvQTF3MjFOwG0> M{DXfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU2Oy9pPmPBUmdGWjxxYU6=
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NCI-H1355 MlLJS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHzZc4JKSzVyIE2gOFIvQDN7IN88US=> M1myPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU2Oy9pPmPBUmdGWjxxYU6=
D-247MG NXvZV5Y4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mlv2TWM2OCB;IES1MlcyQSEQvF2= Mo[1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVU{Nyd-U1HOS2VTRC:jPh?=
MC-CAR NH7qN5FIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MUnJR|UxKD1iNEWuPVY6OSEQvF2= MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1OVMwLz6VQV7HSXI9N2F-
EW-1 M4\hemdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVvJR|UxKD1iNEeuOVYzPCEQvF2= Mn7DQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVU{Nyd-U1HOS2VTRC:jPh?=
GI-ME-N NXPTdWtOT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3;zPGlEPTBiPTC0PE4yOzh2IN88US=> M2LrNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU2Oy9pPmPBUmdGWjxxYU6=
BT-474 NWfoWHp6T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXrJR|UxKD1iNEiuNVc{QCEQvF2= M4rMVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU2Oy9pPmPBUmdGWjxxYU6=
LB373-MEL-D NX3DcGpUT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnXhTWM2OCB;IES4Mlc2PjNizszN M1vxTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU2Oy9pPmPBUmdGWjxxYU6=
Assay
Methods Test Index PMID
Western blot p-Met / Met / p-Axl / Axl / pERK / ERK / pEGFR / EGFR / p-STAT3 / STAT3 / p-Akt / Akt ; p-Raf-1 / Raf-1 / p-MEK / MEK ; cleaved PARP / PARP ; p27 / pS10-p27 / pT157-p27 / pT187-p27 ; Bcl-2 / Bcl-xl / Mcl-1 / Bax / Bak / Bad / Bim EL / PUMA 28604685 27508092 21045138 17927446
Immunofluorescence Bax / Cyto C ; E-cadherin / β-catenin / Vimentin ; EGFR 17927446 19825949 27612423
Growth inhibition assay Cell viability 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 (from reference)

Kinase Assay:[1]
  • 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]
  • 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.
Animal Research:[6]
  • Animal Models: Male 5-week-old BALB-nu/nu with HPAC cells
  • Dosages: 50 mg/kg
  • Administration: Oral administration

Solubility (25°C)

In vitro

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)

Chemical Information

Molecular Weight 429.90
Formula

C22H23N3O4.HCl

CAS No. 183319-69-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles COCCOC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC=CC(=C3)C#C)OCCOC.Cl

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04172779 Not yet recruiting Drug: Erlotinib Hydrochloride Cirrhosis Liver University of Texas Southwestern Medical Center July 2023 Phase 2
NCT03460678 Terminated 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 Suspended Drug: IRX4204|Drug: erlotinib Lung Cancer Nonsmall Cell Io Therapeutics|Dartmouth College May 2016 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-11-29)

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:
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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