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OSI-420

Cat. No. M3491

OSI-420 Structure
Size Price Availability
5mg USD 140 Custom Synthesis
10mg USD 260 Custom Synthesis
50mg USD 680 Custom Synthesis
200mg USD 1480 Custom Synthesis
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

OSI-420 is an active metabolite of erlotinib which is an orally active EGFR tyrosin kinase inhibitor with IC50 of 2 and 20 nM for the inhibition of human EGFR and EGFR autophosphorylation in tumor cells. Erlotinib disappearance from plasma after a short IV infusion was biexponential with a mean terminal half-life of 5.2 h and a mean clearance of 128 ml/min per m2. OSI-420 exposure (AUC) in plasma was 30% (range 12–59%) of erlotinib, and OSI-420 clearance was more than 5-fold higher than erlotinib. Erlotinib and OSI-420 were detectable in CSF. The CSF penetration (AUCCSF:AUCplasma) of erlotinib and OSI-420 was <5% relative to total plasma concentration, but CSF compound exposure was ∼30% of plasma free compound exposure, which was calculated from published plasma protein binding values. The intravenous administration of erlotinib was well tolerated.

Protocol
Cell Experiment
Cell lines A549, H322, H3255, H358 H661, H1650, H1975, H1299, H596 cells
Preparation 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. Using cell count and the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay to assay cell viability . Expressing growth inhibition 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
Concentrations 30 nM-20 μM
Incubation time 72 hour
Animal Experiment
Animal models Male 5-week-old BALB-nu/nu mice with HPAC
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)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 415.87
Formula C21H21N3O4.HCl
CAS Number 183320-51-6
Purity >99%
Solubility DMSO 80 mg/mL
Storage at -20°C
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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: OSI-420 supplier, EGFR/HER2, inhibitors

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