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Erlotinib (CP-358774)

Cat. No. M5621
Erlotinib (CP-358774) Structure
Synonym:

CP358774; NSC 718781; OSI-774

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 50  USD50 In stock
50mg USD 35  USD35 In stock
100mg USD 50  USD50 In stock
500mg USD 75  USD75 In stock
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Quality Control & Documentation
Biological Activity

Erlotinib (CP-358774) is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl. Erlotinib reduces EGFR autophosphorylation in intact tumor cells with an IC50 of 20 nM. Erlotinib is used for the treatment of non-small cell lung cancer.

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.
Chemical Information
Molecular Weight 393.44
Formula C22H23N3O4
CAS Number 183321-74-6
Solubility (25°C) DMSO 60 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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.

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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  Catalog
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Keywords: Erlotinib (CP-358774), CP358774; NSC 718781; OSI-774 supplier, EGFR/HER2, inhibitors, activators


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