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Purity: ≥98%
Erlotinib HCl (formerly OSI-744, OSI744; trade name: Tarceva), the hydrochloride salt of erlotinib, is an EGFR (epidermal growth factor receptor) inhibitor with antitumor activity. In cell-free experiments, it inhibits EGFR with an IC50 of 2 nM, and when compared to human c-Src or v-Abl, it is >1000 times more sensitive to inhibit EGFR. The FDA and other nations have authorized erlotinib, a quinazoline derivative, for the treatment of pancreatic cancer, non-small cell lung cancer (NSCLC), and various other cancer types.
| Targets |
EGFR (IC50 = 2 nM)
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|---|---|
| ln Vitro |
Erlotinib HCl potently inhibits EGFR activation in intact cells, such as MDA MB-468 human breast cancer cells, DiFi human colon cancer cells, and HNS human head and neck tumor cells (IC50 20 nM). DiFi human colon cancer cells undergo apoptosis when exposed to 1 μM erlotinib HCl.[1] With an IC50 ranging from 29 nM to >20 μM, erlotinib inhibits the growth of a panel of NSCLC cell lines, including A549, H322, H3255, H358 H661, H1650, H1975, H1299, and H596.[2] Erlotinib HCl (2 μM) strongly suppresses the proliferation of BxPC-3 and AsPC-1 pancreatic cells.[3] When combined with gemcitabine, the effects of erlotinib HCl are thought to be additive in pancreatic cancer cells that have mutated KRAS. EGFR phosphorylation at the Y845 (Src-dependent phosphorylation) and Y1068 (auto-phosphorylation) sites is inhibited by ten micromolar of erlotinib HCl.[4] When combined with erlotinib HCl, rapamycin-stimulated Akt activity may be down-regulated, and this has a synergistic effect on inhibiting cell growth. [5]
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| ln Vivo |
Erlotinib HCl fully inhibits EGF-induced autophosphorylation of EGFR in human HN5 tumors growing as xenografts in athymic mice, as well as of the treated mice's hepatic EGFR, at doses of 100 mg/kg.[1] H460a and A549 tumor models are inhibited by erlotinib HCl (100 mg/Kg) at 71 and 93% inhibition rates, respectively.[5]
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| Enzyme Assay |
The process of coating 96-well plates involves incubating 100 μL of 0.25 mg/mL PGT in PBS per well for an entire night at 37 °C. Aspiration is used to remove excess PGT, and three washing buffer washes (0.1% Tween 20 in PBS) are performed on the plate. 50 μL of 50 mM HEPES (pH 7.3) containing 0.1 mM sodium orthovanadate, 125 mM sodium chloride, 24 mM magnesium chloride, 20 μM ATP, 1.6 μg/mL EGF, and 15 ng of affinity-purified EGFR from A431 cell membranes is used for the kinase reaction. A final DMSO concentration of 2.5% is achieved by adding erlotinib HCl in DMSO. When ATP is added, phosphorylation begins and continues for eight minutes at room temperature while being constantly shaken.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. In wells without AlP, EGFR, or PGT, the signal for controls is usually between 0.6 and 1.2 absorbance units, with almost no background, and it is proportional to the incubation period of 10 minutes.
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| Cell Assay |
Seeded in triplicate, exponentially growing cells are subjected for 72 hours to serial dilutions of erlotinib, pemetrexed, or the combination at a constant concentration ratio of 4:1. Cell count and the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay are used to measure cell viability. The percentage of drug-treated control cells that survive compared to PBS-treated control cells (which are thought to be 100% viable) is known as growth inhibition. The CalcuSyn software determines the IC50 value, which is the concentration at which a 72-hour exposure to drug(s) results in a 50% inhibition of cell growth when compared to untreated control cells.
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| Animal Protocol |
Mice: Erlotinib (5 mg/kg) is administered p.o. or i.p. to Bcrp1/Mdr1a/1b-/- and WT mice. The selection of i.p. administration is predicated on full bioavailability and optimal drug absorption. Three series of samples are taken from the lateral tail vein tip. Whole blood samples are taken during the first series at 15, min, 0.5, 1.5, 5, and 10 h following injection. The sampling times of the two subsequent series are adjusted to 5 and 15 minutes and 0.5, 1.5, 4, and 8 hours after injection based on the findings of this initial group. Blood samples are collected, centrifuged right away, and the plasma is kept at -20°C until high-performance liquid chromatographic analysis is performed.
Rats: There are male Crl:CD (SD) rats (244-297 g) that are seven weeks old. Erlotinib hydrochloride (10 mg/kg and 20 mg/kg) is given orally to the animals by gavage. |
| References |
| Molecular Formula |
C22H23N3O4.HCL
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|---|---|
| Molecular Weight |
429.90
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| Exact Mass |
429.1455339
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| Elemental Analysis |
C, 61.47; H, 5.63; Cl, 8.25; N, 9.77; O, 14.89
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| CAS # |
183319-69-9
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| Related CAS # |
Erlotinib-d6 hydrochloride;1189953-78-3;Erlotinib;183321-74-6;Erlotinib mesylate;248594-19-6;Erlotinib-13C6 hydrochloride;1210610-07-3;Erlotinib-d6;1034651-23-4
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| Appearance |
White to off-white solid powder
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| SMILES |
COCCOC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC=CC(=C3)C#C)OCCOC.Cl
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| InChi Key |
GTTBEUCJPZQMDZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H23N3O4.ClH/c1-4-16-6-5-7-17(12-16)25-22-18-13-20(28-10-8-26-2)21(29-11-9-27-3)14-19(18)23-15-24-22;/h1,5-7,12-15H,8-11H2,2-3H3,(H,23,24,25);1H
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| Chemical Name |
N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine;hydrochloride
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| Synonyms |
NSC718781 HCl; NSC-718781 HCl; CP358774 HCl, NSC 718781 HCl; CP-358774 HCl; CP 358774 HCl; OSI-774 HCl; OSI 774 HCl; OSI774 HCl; Erlotinib hydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.5 mg/mL (1.16 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 5.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 0.5 mg/mL (1.16 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 5.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: 0.5 mg/mL (1.16 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Solubility in Formulation 4: 15% Captisol: 15 mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3261 mL | 11.6306 mL | 23.2612 mL | |
| 5 mM | 0.4652 mL | 2.3261 mL | 4.6522 mL | |
| 10 mM | 0.2326 mL | 1.1631 mL | 2.3261 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| 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 2024 | Phase 2 |
| NCT02273362 | Active Recruiting |
Drug: Erlotinib Drug: Erlotinib Hydrochloride |
Cirrhosis Hepatocellular Carcinoma |
National Cancer Institute (NCI) |
November 24, 2014 | Phase 1 Phase 2 |
| NCT00076310 | Active Recruiting |
Drug: OSI-774 Drug: Cisplatin |
Head and Neck Cancer | M.D. Anderson Cancer Center | January 28, 2004 | Phase 2 |
| NCT01470716 | Active Recruiting |
Drug: Erlotinib | NSCLC Stage II NSCLC, Stage IIIA |
National Cancer Center, Korea | January 2012 | Phase 2 |
| NCT03110484 | Active Recruiting |
Drug: Pemetrexed 500 MG Drug: Erlotinib |
Biliary Tract Cancer | Samsung Medical Center | July 9, 2021 | Phase 2 |
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