Erlotinib HCl (OSI-744)

Catalog No.S1023

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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Erlotinib HCl (OSI-744) Chemical Structure

Erlotinib HCl (OSI-744) Chemical Structure
Molecular Weight: 429.90

Validation & Quality Control

Cited by 72 publications:

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Quality Control & MSDS

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Product Information

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  • Research Area
  • Combination Therapy
    Combination Therapy

Product Description

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)
IC50 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]
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]
Features

Protocol(Only for 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 Assay: [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 Study: [6]

Animal Models Male 5-week-old BALB-nu/nu with HPAC cells
Formulation 6% Captisol
Dosages 50 mg/kg
Administration Oral administration

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Moyer JD, et al. Cancer Res. 1997, 57(21), 4838-4848.

[2] Li T, et al. Clin Cancer Res, 2007, 13(11), 3413-3422.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-30)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02795884 Not yet recruiting NSCLC Yonsei University June 2016 Phase 3
NCT02770014 Not yet recruiting Epidermal Growth Factor Receptor|Non-Small Cell Lung Cancer Dana-Farber Cancer Institute|Astellas Pharma Inc June 2016 Phase 2
NCT02689336 Not yet recruiting Glioma|Rhabdomyosarcoma|Osteosarcoma|Medulloblastoma|Neuroectodermal Tumor|Ependymoma|Ewings Sarcoma|Wilms Tumor Washington University School of Medicine May 2016 Phase 2
NCT02775006 Not yet recruiting Carcinoma, Non-small Cell Lung The Netherlands Cancer Institute|Dutch Society of Physici  ...more The Netherlands Cancer Institute|Dutch Society of Physicians for Pulmonology and Tuberculosis May 2016 Phase 3
NCT02759614 Not yet recruiting NSCLC Guangdong Association of Clinical Trials April 2016 Phase 3

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Chemical Information

Download Erlotinib HCl (OSI-744) SDF
Molecular Weight (MW) 429.90
Formula

C22H23N3O4.HCl

CAS No. 183319-69-9
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms (CP358774, NSC 718781) HCl
Solubility (25°C) * In vitro DMSO 4 mg/mL warming (9.3 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 15% Captisol 16 mg/mL warmed
* <1 mg/ml means slightly soluble or insoluble.
* 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 Name N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine hydrochloride

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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