产品
编 号：F193093
分子式：C19H13F5N6
分子量：420.34
分子式：C19H13F5N6
分子量：420.34
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规格
价格
是否有货
10mM*1mL in DMSO
询价
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1mg
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5mg
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10mg
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25mg
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50mg
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CAS No: 1610964-64-1
产品详情
生物活性：
Unesbulin (PTC596) is an orally active and selective B-cell-specific Moloney murine leukemia virus integration site 1 (BMI-1) inhibitor. Unesbulin downregulates MCL-1 and induces p53-independent mitochondrial apoptosis in acute myeloid leukemia (AML) cells. Unesbulin has anti-leukemic activity.
体内研究：
Unesbulin (PTC596; 5?mg/kg; oral gavage; every 3 days for 13 days) significantly prolongs mouse survival. Unesbulin (20?mg/kg; oral gavage; once a week for 15 days) causes tumor volume significantly smaller than that of control SCID mice with K562 cells. Unesbulin (10 or 12.5 ?mg/kg; oral gavage; twice a week until death) causes the survival significantly longer than the vehicle-treated group in NOD-SCID mice with HL-60 cells. Animal Model:NOD-SCID/IL2Rγ-KO (NSG) mice with MOLM-13 cells
Dosage:5?mg/kg
Administration:Oral gavage; every 3 days for 13 days
Result:Significantly prolonged mouse survival compared with the vehicle-treated mice in a dose-dependent manner.
体外研究：
Unesbulin (PTC596; 20-200?nM; for 48?hours) induces apoptosis in AML cells in a p53-independent manner. BMI-1 overexpression desensitizes AML cells to PTC596-induced apoptosis. Unesbulin (200?nM; for 10?hours) leads to an accumulation of cells in G2/M phase. Unesbulin (0.012-1 μM; for 20?hours) significantly reduces protein levels of BMI-1. Unesbulin inhibits APC/CCDC20 activity resulting in the persistent activation of CDK1 and CDK2 which mediate the hyperphosphorylation of BMI1.
Unesbulin (PTC596) is an orally active and selective B-cell-specific Moloney murine leukemia virus integration site 1 (BMI-1) inhibitor. Unesbulin downregulates MCL-1 and induces p53-independent mitochondrial apoptosis in acute myeloid leukemia (AML) cells. Unesbulin has anti-leukemic activity.
体内研究：
Unesbulin (PTC596; 5?mg/kg; oral gavage; every 3 days for 13 days) significantly prolongs mouse survival. Unesbulin (20?mg/kg; oral gavage; once a week for 15 days) causes tumor volume significantly smaller than that of control SCID mice with K562 cells. Unesbulin (10 or 12.5 ?mg/kg; oral gavage; twice a week until death) causes the survival significantly longer than the vehicle-treated group in NOD-SCID mice with HL-60 cells. Animal Model:NOD-SCID/IL2Rγ-KO (NSG) mice with MOLM-13 cells
Dosage:5?mg/kg
Administration:Oral gavage; every 3 days for 13 days
Result:Significantly prolonged mouse survival compared with the vehicle-treated mice in a dose-dependent manner.
体外研究：
Unesbulin (PTC596; 20-200?nM; for 48?hours) induces apoptosis in AML cells in a p53-independent manner. BMI-1 overexpression desensitizes AML cells to PTC596-induced apoptosis. Unesbulin (200?nM; for 10?hours) leads to an accumulation of cells in G2/M phase. Unesbulin (0.012-1 μM; for 20?hours) significantly reduces protein levels of BMI-1. Unesbulin inhibits APC/CCDC20 activity resulting in the persistent activation of CDK1 and CDK2 which mediate the hyperphosphorylation of BMI1.
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