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LY900009

Cat. No. M2828
LY900009 Structure
Size Price Availability Quantity
5mg USD 160  USD160 In stock
10mg USD 250  USD250 In stock
25mg USD 500  USD500 In stock
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Quality Control & Documentation
Biological Activity

LY900009 is a potent and orally active, first-in-class inhibitor of Notch signaling via selective inhibition of the γ-secretase protein (GSI). LY900009 inhibited Notch signalling in tumor cell lines and endothelial cells (IC50 range: 0.005-20 nM).

Chemical Information
Molecular Weight 409.48
Formula C23H27N3O4
CAS Number 209984-68-9
Solubility (25°C) DMSO
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] Shubham Pant, et al. A first-in-human phase I study of the oral Notch inhibitor, LY900009, in patients with advanced cancer

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  Catalog
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Keywords: LY900009 supplier, Notch, inhibitors, activators


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