YZ-35
YZ-35 is a STAT3 inhibitor, with a Ki value of 0.38 μM. YZ-35 binds directly to STAT3 with high affinity, exhibiting a dissociation constant (Kd) of 190 nM. YZ-35 directly attenuates the dual phosphorylation of STAT3 (Tyr705 and Ser727). YZ-35 suppresses colony formation, cellular migration, and induces apoptosis in breast cancer cell lines (BCSC). YZ-35 selectively suppresses BCSC self-renewal. YZ-35 inhibits tumor growth in the BCSC xenograft models. YZ-35 can be used for the study of breast cancer.
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- Fòrmula: C29H24N2O5S
- Peso molecular:512.58
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
YZ-35 (0.1-100 μM, 48 h) demonstrates inhibitory potency against MDA-MB-231 cells (IC50 = 0.63 μM), MCF-7 cells (IC50 = 0.32 μM) and MCF-10A cells (IC50 = 34.34 μM)[1]. YZ-35 (0-4 μM, 0-48 h) directly attenuates the dual phosphorylation of STAT3 (Tyr705 and Ser727) to exhibit potent anti-breast cancer efficacy efficacy in MDA-MB-231 and MCF-7 cells[1]. YZ-35 (0-6 μM, 24-48 h) suppresses colony formation, cellular migration, and induces apoptosis in MDA-MB-231 and MCF-7 cells[1]. YZ-35 (2.5-10 μM, 48 h) reduces tumor stemness in MDA-MB-231 and MCF-7 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231 cells, MCF-7 cells and MCF-10A cells
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Concentration:0.1-100 μM
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Incubation Time:48 h
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Result:Demonstrated inhibitory potency against MDA-MB-231 cells (IC50 = 0.63 μM), MCF-7 cells (IC50 = 0.32 μM) and MCF-10A cells (IC50 = 34.34 μM).
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Cell Line:MDA-MB-231 cells and MCF-7 cells
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Concentration:0, 1, 2, 3, 4 μM
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Incubation Time:0, 12, 24, 36, 48 h
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Result:Exhibited concentration- and time-dependent suppression of the phosphorylation of STAT3 at both Tyr705 and Ser727 residues in MDA-MB-231 and MCF-7 cell lines, while maintaining total STAT3 protein levels. Showed no effect on the expression levels of STAT1 and STAT5 or their phosphorylation.
Did not impact the phosphorylation of JAK2, Src, and ERK. Inhibited the expression of critical apoptosis-related proteins, including Cyclin D1, BCL2, BCL-xL, and Survivin, in a concentration-dependent manner.
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Cell Line:MDA-MB-231 cells and MCF-7 cells
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Concentration:0, 1, 2, 3 μM
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Incubation Time:24 h
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Result:Decreased the migration of MDA-MB-231 cells by 99%. Reduced the migration in MCF-7 cells by 72.97%.
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Cell Line:MDA-MB-231 cells and MCF-7 cells
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Concentration:0, 1, 2, 4, 6 μM
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Incubation Time:48 h
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Result:Induced programmed cell apoptosis in a concentration-dependent manner, with differential responses observed between BRCA subtypes: predominantly late-stage apoptosis in MDA-MB-231 cells, while promoting both earlyand late-phase apoptotic events in MCF-7 cells.
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Cell Line:MDA-MB-231 cells and MCF-7 cells
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Concentration:0, 1, 2, 3 μM
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Incubation Time:48 h
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Result:Induced programmed cell death of BRCA, notably manifesting as pronounced chromatin condensation and nuclear fragmentation, with the most substantial apoptotic phenotype observed at 3 μM concentration.
| Species | Dose | Route | AUC0-t | AUC0-∞ | T1/2 | MRT0-∞ | Vd/F | CL |
|---|---|---|---|---|---|---|---|---|
| Mice[1] | 10 mg/kg | i.v. | 6637.79 ng·h/mL | 7213.53 ng·h/mL | 16.03 h | 9.92 h | 31.01 L/kg | 1.41 L/h/kg |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:1 × 107 MDA-MB-21 cells were resuspended with 100 μL saline and injected into the left flank of 5-week-old female BALB/c-nude mice[1]
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Dosage:5, 10 mg/kg
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Administration:i.v. once daily for 21 days
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Result:Inhibited tumor growth (the TGI of high (10 mg/kg) and low (5 mg/kg) groups were 89.98 and 74.13%, respectively). Inhibited STAT3 phosphorylation and significantly reduced FOXM1 and AURKA expression. Augmented the proportion of apoptotic cells while concurrently diminishing Ki67-positive proliferating cell populations in tumor tissues relative to vehicle controls. Showed no significant toxicity was observed in major organs including the heart, liver, spleen, lung, and kidney.
Chemical Information
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Peso molecular 512.58
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Fòrmula C29H24N2O5S
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SMILES
O=C(CC1=CC2=C(C=CC=C2)N1)NCC(C3=O)=C(C(C4=C3C=CC=C4OC)=O)SC5=CC=C(C=C5)OC
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
YZ-35 Related Classifications
HY-175253 Related Classifications
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