Gal-ARV-771
Gal-ARV-771 is a galactose-modified derivative of ARV-771 (HY-100972). Gal-ARV-771 is activated in cells expressing SA-β-Gal, thereby releasing ARV-771. Gal-ARV-771 selectively induces Apoptosis. ARV-771 is a BET PROTAC degrader. Gal-ARV-771 can be used in the research of lung adenocarcinoma (Gal+linker: Gal-PAB (HY-188142); PROTAC: ARV-771 (HY-100972)).
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- CAS No.: 3055593-64-8
- Formule: C71H84ClN9O19S2
- Masse moléculaire:1467.06
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Pureté et documentation
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Activité biologique
Description
IC50 & Target
[1]|
BRD4 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
3.29 μM
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Inhibition of cell viability against normal non-senescent A549 human lung adenocarcinoma cells incubated for 72 hrs by CCK-8 assay.
Inhibition of cell viability against normal non-senescent A549 human lung adenocarcinoma cells incubated for 72 hrs by CCK-8 assay.
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38635879 |
| A549 | IC50 |
640 nM
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Inhibition of cell viability against etoposide-induced senescent A549 human lung adenocarcinoma cells incubated for 72 hrs by CCK-8 assay.
Inhibition of cell viability against etoposide-induced senescent A549 human lung adenocarcinoma cells incubated for 72 hrs by CCK-8 assay.
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38635879 |
In Vitro
Gal-ARV-771 (100 μM; 16-24 h) is stable for 24 h in full cell culture medium, and is fully converted to active ARV-771 after 16 h of combined action of esterase and β-galactosidase[1].
Gal-ARV-771 (72 h) shows potent selective cytotoxicity towards senescent A549 cells with 5.17-fold higher activity relative to non-senescent A549 cells, with an IC50 of 640 nM for senescent A549 cells[1].
Gal-ARV-771 (1 μM; 24 h) induces selective apoptosis in senescent A549 cells, with minimal induction of apoptosis in non-senescent A549 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Normal non-senescent A549 (n-A549) and etoposide-induced senescent A549 (s-A549) human lung adenocarcinoma cells
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Concentration:Serial concentrations
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Incubation Time:72 h
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Result:Exhibits an IC50 of 3.29 μM for normal A549 cells and 640 nM for senescent A549 cells, producing a senolytic index of 5.17 between normal and senescent A549 cells.
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Cell Line:Normal A549 (n-A549) and etoposide-induced senescent A549 (s-A549) human lung adenocarcinoma cells
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Concentration:1 μM
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Incubation Time:24 h
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Result:Causes 8.07% of normal non-senescent A549 cells to undergo early apoptosis.
Causes 16.7% of etoposide-induced senescent A549 cells to undergo early apoptosis.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD.Cg-Prkdcscid/J (female, 5 weeks old, severe combined immunodeficient, SCID)[1]
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Dosage:20 mg/kg
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Administration:i.p.; 5 days on / 2 days off; 19 days
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Result:Produced a 74% tumor growth inhibition (TGI) when administered in combination with etoposide.
Did not produce comparable tumor growth inhibition as a single agent.
Significantly reduced tumor BRD4 protein expression levels when combined with etoposide.
Reduced tumor cell proliferation as measured by Ki-67 staining when combined with etoposide.
Increased apoptosis as measured by cleaved caspase-3 staining when combined with etoposide.
Reduced expression of the senescent biomarker p21 in tumors compared to etoposide alone when combined with etoposide.
Showed no significant toxicity, as evidenced by stable body weights throughout the study period.
Chemical Information
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CAS No. 3055593-64-8
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Masse moléculaire 1467.06
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Formule C71H84ClN9O19S2
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SMILES
O=C(N[C@@H](C)C1=CC=C(C=C1)C2=C(N=CS2)C)[C@H]3N(C[C@@H](C3)OC(OCC4=CC=C(O[C@@H]([C@@H]5OC(C)=O)O[C@H](COC(C)=O)[C@H](OC(C)=O)[C@@H]5OC(C)=O)C=C4)=O)C([C@H](C(C)(C)C)NC(COCCCOCCNC(C[C@@H]6N=C(C7=C(N8C(C)=NN=C68)SC(C)=C7C)C9=CC=C(C=C9)Cl)=O)=O)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Gal-ARV-771 Related Classifications
HY-158331 Related Classifications
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