OY-101
OY-101 is an orally active, potent and specific P-glycoprotein (P-gp) inhibitor. OY-101 can sensitize drug-resistant tumors and effectively reverse tumor multidrug resistance. OY-101 is improvements in water-solubility, cytotoxicity, and reversal activity compared to Tetrandrine (HY-13764).
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- No. CAS: 41183-02-2
- Fòrmula: C27H31NO4
- Peso molecular:433.54
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Almacenamiento:
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Actividad biológica
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| ECa-109 cell line | IC50 |
>100 μM
Compound: 39; OY-101
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Cytotoxicity against human Eca-109 cells incubated for 48 hrs by CCK-8 method
Cytotoxicity against human Eca-109 cells incubated for 48 hrs by CCK-8 method
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[PMID: 36892076] |
| ECa-109 cell line | IC50 |
1872 nM
Compound: 39; OY-101
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Reversal of VCR -resistance in human Eca-109 cells assessed as cell viability at 1 uM incubated for 48 hrs by CCK-8 method (Rvb = 6830.0+/-537.0 nM)
Reversal of VCR -resistance in human Eca-109 cells assessed as cell viability at 1 uM incubated for 48 hrs by CCK-8 method (Rvb = 6830.0+/-537.0 nM)
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[PMID: 36892076] |
| ECa-109 cell line | IC50 |
66.1 nM
Compound: 39; OY-101
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Reversal of VCR -resistance in human Eca-109 cells assessed as cell viability at 2.5 uM incubated for 48 hrs by CCK-8 method (Rvb = 6830.0+/-537.0 nM)
Reversal of VCR -resistance in human Eca-109 cells assessed as cell viability at 2.5 uM incubated for 48 hrs by CCK-8 method (Rvb = 6830.0+/-537.0 nM)
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[PMID: 36892076] |
| ECa-109 cell line | IC50 |
9.9 nM
Compound: 39; OY-101
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Reversal of VCR -resistance in human Eca-109 cells assessed as cell viability at 5 uM incubated for 48 hrs by CCK-8 method (Rvb = 6830.0+/-537.0 nM)
Reversal of VCR -resistance in human Eca-109 cells assessed as cell viability at 5 uM incubated for 48 hrs by CCK-8 method (Rvb = 6830.0+/-537.0 nM)
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[PMID: 36892076] |
| GES1 | IC50 |
>50 μM
Compound: 39; OY-101
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Cytotoxicity against human GES1 cells incubated for 48 hrs by CCK-8 method
Cytotoxicity against human GES1 cells incubated for 48 hrs by CCK-8 method
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[PMID: 36892076] |
| HEK-293T | IC50 |
>50 μM
Compound: 39; OY-101
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Cytotoxicity against HEK293T cells incubated for 48 hrs by CCK-8 method
Cytotoxicity against HEK293T cells incubated for 48 hrs by CCK-8 method
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[PMID: 36892076] |
| HK-2 | IC50 |
>50 μM
Compound: 39; OY-101
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Cytotoxicity against human HK-2 cells incubated for 48 hrs by CCK-8 method
Cytotoxicity against human HK-2 cells incubated for 48 hrs by CCK-8 method
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[PMID: 36892076] |
| LX-2 | IC50 |
>50 μM
Compound: 39; OY-101
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Cytotoxicity against human LX2 cells incubated for 48 hrs by CCK-8 method
Cytotoxicity against human LX2 cells incubated for 48 hrs by CCK-8 method
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[PMID: 36892076] |
OY-101 shows excellent synergistic anti-cancer effect with Vincristine (HY-N0488A) against drug-resistant cells Eca109/VCR, with an IC50 of 9.9 ± 1.3 nM[1].
OY-101 (0-5 μM) is not significantly toxic to Eca109/VCR cells, and exhibits significantly increased Vincristine (HY-N0488A) sensitization in Eca109/VCR cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Eca109/VCR cells
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Concentration:1.0, 2.5, and 5.0 μM
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Incubation Time:48 h
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Result:Exhibited significantly increased Vincristine sensitization in Eca109/VCR cells, achieving around 3.7, 103.4, and 690.6-fold reversal activity, respectively.
OY-101 (Intravenous (3 mg/kg) and oral administration (30 mg/kg); once) shows good pharmacokinetics[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female nude mice (4-5 weeks old, xenograft model bearing P-gp-overexpressing Eca109/VCR cells)[1]
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Dosage:30 mg/kg
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Administration:IG, once every 2 days, for 3 weeks, 1 h before tail vein injection of Vincristine (HY-N0488A)
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Result:Only co-administration OY-101 with Vincristine can effectively inhibit tumor proliferation in vivo (P < 0.001) and significantly reduce tumor weight. After 3 weeks of treatment, the tumor growth inhibition rate of the OY-101/Vincristine combination was 79.13%, which was significantly lower than that of the single-treatment group and the vehicle group.
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Animal Model:SD rats (8 week-old, male, 300-400 g)[1]
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Dosage:3 mg/kg (IV), 30 mg/kg (PO)
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Administration:Intravenous and oral administration, once (Pharmacokinetic Analysis)
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Result:Pharmacokinetic Parameters of OY-101 in male Sprague-Dawley rats[1].
IV (3 mg/kg) PO (30 mg/kg) Tmax (h) 0.17 ± 0.12 0.38 ± 0.18 Cmax (ng/mL) 1573.20 ± 143.97 636.55 ± 355.60 AUC0-t (ng/mL∗h) 2688.45 ± 180.10 2665.45 ± 450.92 t1/2 (h) 8.43 ± 7.83 7.37 ± 4.92 CL/F (L/kg/h) 1.10 ± 0.08 11.16 ± 2.10 Vz/F (L/kg) 12.84 ± 11.33 111.27 ± 56.82 F (%) 7.65 ± 2.15