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Erlotinib

Cat. No. M5621

Erlotinib Structure

Synonym: CP358774, NSC 718781

Size Price Availability Quantity
100mg USD 80 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Erlotinib is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl.

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 393.44
Formula C22H23N3O4
CAS Number 183321-74-6
Purity >99%
Solubility 78 mg/mL in DMSO
Storage at -20°C
Customer Product Validation
Source Sci Rep (2017). Figure 1. Erlotinib (AbMole Bioscience, Houston, TX)
Method bacterial cell wall-induced lipolysis
Cell Lines Murine 3T3-L1 preadipocytes
Concentrations 1–10 μM
Incubation Time 48 h
Results FK565-stimulated glycerol release was lower in 3T3-L1 adipocytes pre-incubated with TKIs ponatinib, dasatinib, dafabranib, vandetanib, ruxolitinib, SB203580, ibrutinib, gefitinib, sorafenib, neratinib, erlotinib, at 1–10 μM.
Rating
Product Citations
References

First-line erlotinib versus gemcitabine/cisplatin in patients with advanced EGFR mutation-positive non-small-cell lung cancer: analyses from the phase III, randomized, open-label, ENSURE study.
Wu YL, et al. Ann Oncol. 2015 Sep;26(9):1883-9. PMID: 26105600.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Erlotinib, CP358774, NSC 718781 supplier, EGFR/HER2, inhibitors

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