产品
编 号：F527519
分子式：C25H32N4O7S
分子量：532.61
分子式：C25H32N4O7S
分子量：532.61
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规格
价格
是否有货
10mM*1mL in DMSO
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1mg
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5mg
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10mg
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50mg
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100mg
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结构图
CAS No: 935888-69-0
产品详情
生物活性：
Oprozomib (PR-047) is an orally bioavailable and selective peptide epoxyketone proteasome inhibitor with IC50s of 36 and 82 nM for proteasome (β5) and immunoproteasome (LMP7), respectively. Oprozomib (ONX 0912) induces apoptosis in MM cells.
体内研究：
Oprozomib (PR-047) selectively inhibits chymotrypsin-like (CT-L) activity of both the constitutive proteasome (β5) and immunoproteasome (LMP7) and demonstrates an absolute bioavailability of up to 39% in rodents and dogs.Oprozomib promotes antitumor activity in multiple animal models by oral administration at doses below the maximum tolerated dose (MTD). Oprozomib (30?mg/kg by oral gavage once daily for 5 consecutive days followed by 2 days of rest) treatment decreases tumor burden in C57Bl/6 and NOD.SCID.IL2Rγ-/- mice.Animal Model:C57Bl/6 and NOD.SCID.IL2Rγ-/- mice bearing established human RPMI-8226-luc myeloma cells
Dosage:30?mg/kg
Administration:Oral gavage once daily for 5 consecutive days followed by 2 days of rest
Result:Decreased human MM tumor burden and protects mice from bone destruction.
体外研究：
Oprozomib inhibits 20S chymotrypsin-like (CT-L) with an IC50 of 55?±?19?nM. Oprozomib inhibits human leukemia Molt-4 cells CT-L with an IC50 of 66 nM.Oprozomib (ONX 0912; 1-1000 nM; 48 hours) significantly decreases the viability of human multiple myeloma (MM) cell lines.The anti-MM activity of Oprozomib is associated with activation of caspase-8, caspase-9, caspase-3, and PARP.
Oprozomib (PR-047) is an orally bioavailable and selective peptide epoxyketone proteasome inhibitor with IC50s of 36 and 82 nM for proteasome (β5) and immunoproteasome (LMP7), respectively. Oprozomib (ONX 0912) induces apoptosis in MM cells.
体内研究：
Oprozomib (PR-047) selectively inhibits chymotrypsin-like (CT-L) activity of both the constitutive proteasome (β5) and immunoproteasome (LMP7) and demonstrates an absolute bioavailability of up to 39% in rodents and dogs.Oprozomib promotes antitumor activity in multiple animal models by oral administration at doses below the maximum tolerated dose (MTD). Oprozomib (30?mg/kg by oral gavage once daily for 5 consecutive days followed by 2 days of rest) treatment decreases tumor burden in C57Bl/6 and NOD.SCID.IL2Rγ-/- mice.Animal Model:C57Bl/6 and NOD.SCID.IL2Rγ-/- mice bearing established human RPMI-8226-luc myeloma cells
Dosage:30?mg/kg
Administration:Oral gavage once daily for 5 consecutive days followed by 2 days of rest
Result:Decreased human MM tumor burden and protects mice from bone destruction.
体外研究：
Oprozomib inhibits 20S chymotrypsin-like (CT-L) with an IC50 of 55?±?19?nM. Oprozomib inhibits human leukemia Molt-4 cells CT-L with an IC50 of 66 nM.Oprozomib (ONX 0912; 1-1000 nM; 48 hours) significantly decreases the viability of human multiple myeloma (MM) cell lines.The anti-MM activity of Oprozomib is associated with activation of caspase-8, caspase-9, caspase-3, and PARP.
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