Autophinib

Catalog No.S8596 Batch:S859601

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Technical Data

Formula

C14H11ClN6O3
Molecular Weight 346.73 CAS No. 1644443-47-9
Solubility (25°C)* In vitro DMSO 5 mg/mL (14.42 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
0.25mg/ml 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 95% Corn oil
0.25mg/ml 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. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description 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.
Targets
Vps34 [1] Autophagy [1]
(Rapamycin induced)		 Autophagy [1]
(starvation-induced)
19 nM 40 nM 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 it is not a late stage autophagy inhibitor but an inhibitor of autophagosome formation. 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[1].

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    HeLa cells

  • Concentrations

    30 μM

  • Incubation Time

    18 h

  • Method

    --

Selleck's Autophinib has been cited by 10 publications

Targeting autophagy overcomes cancer-intrinsic resistance to CAR-T immunotherapy in B-cell malignancies [ Cancer Commun (Lond), 2024, 44(3):408-432] PubMed: 38407943
Targeting autophagy overcomes cancer-intrinsic resistance to CAR-T immunotherapy in B-cell malignancies [ Cancer Commun (Lond), 2024, 44(3):408-432] PubMed: 38407943
Activating autophagy promotes skin regeneration induced by mechanical stretch during tissue expansion [ Burns Trauma, 2024, 12:tkad057] PubMed: 38328438
Kaempferol promotes non-small cell lung cancer cell autophagy via restricting Met pathway [ Phytomedicine, 2023, 10.1016/j.phymed.2023.155090] PubMed: 37738907
Genome-wide CRISPR screening identifies TMEM106B as a proviral host factor for SARS-CoV-2 [ Nat Genet, 2021, 53(4):435-444] PubMed: 33686287
17β-Estradiol Enhances Porcine Meiosis Resumption from Autophagy-Induced Gap Junction Intercellular Communications and Connexin 43 Phosphorylation via the MEK/ERK Signaling Pathway [ J Agric Food Chem, 2021, 69(40):11847-11855] PubMed: 34609142
17β-estradiol improves the developmental ability, inhibits reactive oxygen species levels and apoptosis of porcine oocytes by regulating autophagy events [ J Steroid Biochem Mol Biol, 2021, 209:105826] PubMed: 33581253
Identification of Required Host Factors for SARS-CoV-2 Infection in Human Cells [ Cell, 2020, S0092-8674(20)31394-5] PubMed: 33147445
Antileukemic activity of the VPS34-IN1 inhibitor in acute myeloid leukemia [ Oncogenesis, 2020, 9(10):94] PubMed: 33093450
Stimulation of Hair Growth by Small Molecules that Activate Autophagy [ Cell Rep, 2019, 27(12):3413-3421] PubMed: 31216464

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.