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Autophinib Autophagy inhibitor

Cat.No.S8596

Autophinib is a potent autophagy inhibitor with a novel chemotype with IC50 values of 90 and 40 nM for autophagy in starvation induced autophagy assay and rapamycin induced autophagy assay. The IC50 value for Vps34 is 19 nM in vitro.
Autophinib Autophagy inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 346.73

Quality Control

Batch: S859601 DMSO]5 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.60%
99.60

Chemical Information, Storage & Stability

Molecular Weight 346.73 Formula

C14H11ClN6O3

Storage (From the date of receipt)
CAS No. 1644443-47-9 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CC1=CC(=NN1)NC2=CC(=NC(=N2)OC3=CC=C(C=C3)[N+](=O)[O-])Cl

Solubility

In vitro
Batch:

DMSO : 5 mg/mL (14.42 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Mechanism of Action

Targets/IC50/Ki
Vps34 [1]
19 nM
Autophagy [1]
(Rapamycin induced)
40 nM
Autophagy [1]
(starvation-induced)
90 nM
In vitro
Autophinib inhibits the accumulation of autophagosomes under fed as well as starved conditions, but does not affect the number of autolysosomes. Thus this compound is not a late stage autophagy inhibitor but an inhibitor of autophagosome formation. It targets VPS34 but not other lipid kinases, mTOR and TBK1. This chemical appears to be ATP-competitive, targets VPS34 in cell lysate and induces cellular phenotypes consistent with VPS34 inhibition[1].
References

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