Erlotinib HCl (OSI-744)
Catalog No.S1023 Synonyms: (CP358774, NSC 718781) HCl
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.
Cited by 94 Publications
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|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.|
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.  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.  Erlotinib HCl(2 μM) significantly inhibits growth of AsPC-1 and BxPC-3 pancreatic cells.  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.  Combination with Erlotinib HCl could down-modulate rapamycin-stimulated Akt activity and produces a synergistic effect on cell growth inhibition. 
|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.  Erlotinib HCl (100 mg/Kg) inhibits H460a and A549 tumor models with 71 and 93% inhibition rate. |
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.
-  Moyer JD, et al. Cancer Res. 1997, 57(21), 4838-4848.
-  Li T, et al. Clin Cancer Res, 2007, 13(11), 3413-3422.
-  Ali S, et al. Mol Cancer Ther, 2008, 7(6), 1708-1719.
|In vitro||DMSO||4 mg/mL warmed (9.3 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
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.
|Synonyms||(CP358774, NSC 718781) HCl|
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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|
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
Whether S1023 is suitable for mouse assays?
Dissolving S1023 in 15% Captisol is for oral gavage and it's a suspension.