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AG 879

Cat. No. M3098
AG 879 Structure
Synonym:

Tyrphostin AG 879

Size Price Availability Quantity
5mg USD 48  USD48 In stock
10mg USD 75  USD75 In stock
25mg USD 180  USD180 In stock
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Quality Control & Documentation
Biological Activity

Tyrphostin AG 879 potently inhibits HER2/ErbB2 with IC50 of 1 μM, 100- and 500-fold higher selective to ErbB2 than PDGFR and EGFR.

Protocol (for reference only)
Cell Experiment
Cell lines MCF-7 cells
Preparation method Growing cells in 96-well plates which is containing 100 μL medium per well. Ten microliters of MTT solution (5 mg/ml in PBS) is added to each well and incubation continued for 4 h at 37 °C. Subsequently, 100 μL 10% SDS in 0.01 M HCl is added. After incubation at 37°C overnight, absorption is measured at 550 nm in an ELISA reader using a reference filter of 690 nm.
Concentrations 20 μM
Incubation time 46 hours
Animal Experiment
Animal models nude mice carrying v-Ha-RAS transformed NIH 3T3 cells
Formulation 30% dimethyl sulfoxide with PBS
Dosages 20 mg/kg
Administration Intraperitoneally administrated on days 3, 5, 7, 10, 12, 14, and 17.
Chemical Information
Molecular Weight 316.46
Formula C18H24N2OS
CAS Number 148741-30-4
Solubility (25°C) DMSO 25 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] Raphael A Zoeller, et al. A cell-based high-throughput screen identifies tyrphostin AG 879 as an inhibitor of animal cell phospholipid and fatty acid biosynthesis

[2] L-I Larsson. Novel actions of tyrphostin AG 879: inhibition of RAF-1 and HER-2 expression combined with strong antitumoral effects on breast cancer cells

[3] Guo-Lei Zhou, et al. Targeting PAK etk.

[4] Hong He, et al. The Tyr-kinase inhibitor AG879, that blocks the ETK-PAK1 interaction, suppresses the RAS-induced PAK1 activation and malignant transformation

[5] H He, et al. Signal therapy for RAS-induced cancers in combination of AG 879 and PP1, specific inhibitors for ErbB2 and Src family kinases, that block PAK activation

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  Catalog
Abmole Inhibitor Catalog




Keywords: AG 879, Tyrphostin AG 879 supplier, EGFR/HER2, inhibitors, activators


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