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Autophinib

Cat. No. M9155
Autophinib Structure
Size Price Availability Quantity
5mg USD 85  USD85 In stock
10mg USD 148  USD148 In stock
25mg USD 300  USD300 In stock
50mg USD 480  USD480 In stock
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Quality Control & Documentation
Biological Activity

Autophinib is a novel potent autophagy inhibitor, inhibiting autophagy induced by starvation or Rapamycin with IC50 values of 90 and 40 nM, targeting the lipid kinase VPS34 with IC50 value of 19 nM in vitro. Autophinib targets VPS34 but not other lipid kinases, mTOR and TBK1. Autophinib appears to be ATP-competitive, targets VPS34 in cell lysate and induces cellular phenotypes consistent with VPS34 inhibition.

Chemical Information
Molecular Weight 346.73
Formula C14H11ClN6O3
CAS Number 1644443-47-9
Solubility (25°C) DMSO: ≥ 22 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] Robke L, et al. Angew Chem Int Ed Engl. Phenotypic Identification of a Novel Autophagy Inhibitor Chemotype Targeting Lipid Kinase VPS34.

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Keywords: Autophinib supplier, Autophagy, inhibitors, activators


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