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ORY-1001

Cat. No. M5213
ORY-1001 Structure
Synonym:

RG-6016

Size Price Availability Quantity
5mg USD 160 In stock
10mg USD 260 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

ORY-1001 (RG-6016) is the only dual KDM1A/LSD1 inhibitor currently being moved forward to Phase I studies, and it is also the only KDM1A inhibitor in development for the treatment of neurodegenerative disease. In THP-1 (MLL-AF9) cells, ORY-1001 results in a time/dose dependent me2H3K4 accumulation at KDM1A target genes and concomitant induction of differentiation markers. ORY-1001 also induces apoptosis in THP-1 and inhibits proliferation and colony formation of MV(4;11) (MLL-AF4) cells. ORY-1001 (<0.020mg/kg, p.o.) leads to significantly reduced tumor growth in rodent MV(4;11) xenografts.

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 303.27
Formula C15H22N2.2HCl
CAS Number 1431326-61-2
Purity >99%
Solubility Water 60 mg/mL
Storage at -20°C
References

KDM1 histone lysine demethylases as targets for treatments of oncological and neurodegenerative disease.
Maes T, et al. Epigenomics. 2015;7(4):609-26. PMID: 26111032.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: ORY-1001, RG-6016 supplier, Histone demethylases, inhibitors

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