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GSK2879552

Cat. No. M5212
GSK2879552 Structure
Size Price Availability Quantity
5mg USD 130 In stock
10mg USD 220 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Cyclopropylamine containing inhibitor of Lysine Demethylase 1 (LSD1), GSK2879552 is a potent, selective, orally bioavailable, mechanism-based irreversible inactivator of LSD1.

A proliferation screen of cell lines representing a number of tumor types indicated that small cell lung carcinoma (SCLC) is sensitive to LSD1 inhibition. The subset of SCLC lines and primary samples that undergo growth inhibition in response to GSK2879552 exhibit DNA hypomethylation of a signature set of probes, suggesting this may be used as a predictive biomarker of activity.

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 364.48
Formula C23H28N2O2
CAS Number 1401966-69-5
Purity >99%
Solubility DMSO 25 mg/mL
Water 40 mg/mL
Storage at -20°C
References

A DNA Hypomethylation Signature Predicts Antitumor Activity of LSD1 Inhibitors in SCLC.
Mohammad HP, et al. Cancer Cell. 2015 Jul 13;28(1):57-69. PMID: 26175415.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: GSK2879552 supplier, Histone demethylases, inhibitors

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