OA-Br-1
OA-Br-1 is an orally active and selective inhibitor of PTP1B with an IC50 value of 7.08 μM. OA-Br-1 induces apoptosis. OA-Br-1 has broad spectrum anti-proliferative activity against cancer cells, and plays an anti-breast cancer role through the PTP1B/PI3K/AKT signaling pathway both in vitro and in vivo.
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- Formule: C43H70BrNO8
- Masse moléculaire:808.92
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
IC50: PTP1B (7.08 μM)[1]
OA-Br-1 shows stronger inhibitory activity against PTP1B with an IC50 value of 7.08 μM, and weak inhibitory activity against TCPTP, with an IC50 value of 222.28μM[1].
OA-Br-1 (24-72 h) inhibits the proliferation of breast cancer cells in a concentration- and time-dependent manner, with IC50 values on MCF-7, MDA-MB-231 and MDA-MB-453 after 72 h were 8.76, 18.13, and 22.34 μM, respectively[1].
OA-Br-1 (5-30 μM; 48 h) induces apoptosis in MCF-7 and MDA-MB-231 cells[1].
OA-Br-1 increases the thermal stability of PTP1B[1].
OA-Br-1 (5-30 μM; 48 h) decreases the community formed by MCF-7 and MDA-MB-231 cell clones in dose-dependent manner[1].
OA-Br-1 (5-30 μM; 48 h) decreases the protein levels of p-PI3K and p-AKT, exerts its antitumor effects through the PTP1B/PI3K/AKT signaling pathway in breast cancer cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7, MDA-MB-231
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Concentration:5, 10, 20 μM in MCF-7, 10, 20, 30 μM in MDA-MB-231
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Incubation Time:48 h
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Result:The community formed by the two cell clones decreased significantly in dose-dependent manner.
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Cell Line:MCF-7, MDA-MB-231
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Concentration:5, 10, 20, 30 μM
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Incubation Time:48 h
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Result:Cells began to show chromatin aggregation, green fluorescence spots, and a few red fluorescence, indicating most cells to enter the early apoptosis stage.
With the continuous increase concentration, the nucleus and chromatin further contracted and aggregated, the proportion of cells with red fluorescence increased, and most cells entered the late apoptotic stage and died.
Induced apoptosis of most breast cancer cells at 20 μM.
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Cell Line:MCF-7 cells
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Concentration:5, 10, 20, 30 μM
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Incubation Time:48 h
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Result:Inhibited PTP1B protein expression in a concentration-dependent manner in MCF-7 cells.
Decreased the protein levels of p-PI3K and p-AKT.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c female nude mice (4 weeks old and weighing around 18 g) (5 x 106 MCF-7 cells in 200 μL FBS-free medium were subcutaneously injected into the left axilla)[1]
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Dosage:30, 60 mg/kg
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Administration:Intragastric gavage (i.g.); every day
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Result:Tumor growth, volume, and weight were inhibited, with no observed toxicity on body weight or major organ weight indices.
Suppressed the expression of PTP1B, as well as the phosphorylation level of PI3K and AKT protein in the tumor.
Chemical Information
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Masse moléculaire 808.92
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Formule C43H70BrNO8
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SMILES
BrC[C@H]1O[C@H](O[C@@H]2C(C)(C)[C@@](CC[C@]3(C)[C@]4([H])CC=C5[C@@]3(C)CC[C@]6(C(NCCCCCC(OC)=O)=O)[C@@]5([H])CC(C)(C)CC6)([H])[C@]4(C)CC2)[C@@H](O)[C@@H](O)[C@@H]1O
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Synonyms
3-O-(6-Bromo-D-mannosyl)-28-acylamino-n-caproate methyl oleanolic acid
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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)
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