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Autophinib Autophagy inhibitor

Name: Autophinib
Brand: Selleck Chemicals
SKU: S8596
Rating: 5 (9 reviews)

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.

Chemical Structure

Molecular Weight: 346.73

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Quality Control

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

Cited in Nature Medicine for its top-tier quality
COA
SDS
Datasheet

99.60

Related Targets	CXCR Nrf2 Mitophagy LRRK2 ULK FKBP Heme Oxygenase cGAS LC3 Cell wall
Other Autophagy Inhibitors	Resveratrol (trans-Resveratrol) Spautin-1 PIK-III DC661 Lys05 Trihydrochloride Spermidine SMER28 EN6 Flubendazole ROC-325

Chemical Information, Storage & Stability

Molecular Weight	346.73	Formula	C₁₄H₁₁ClN₆O₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1644443-47-9	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
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
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.250mg/ml (0.72mM)	Taking the 1 mL working solution as an example, add 50 μL of 5 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.250mg/ml (0.72mM)	Taking the 1 mL working solution as an example, add 50 μL of 5 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	Vps34 19 nM Autophagy (Rapamycin induced) 40 nM Autophagy (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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/28544137/

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