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Erlotinib

Cat. No. M5621
Erlotinib Structure
Synonym:

CP358774, NSC 718781

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
50mg USD 40  USD40 In stock
100mg USD 60  USD60 In stock
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Quality Control
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.

Product Citations
Customer Product Validations & Biological Datas
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.
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 393.44
Formula C22H23N3O4
CAS Number 183321-74-6
Purity 99.20%
Solubility 65 mg/mL in DMSO
Storage at -20°C
References

[1] Wu YL, et al. Ann Oncol. 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.

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

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