Oprozomib奥泼佐米,935888-69-0

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Oprozomib

CAS No. : 935888-69-0

MCE 国际站：Oprozomib

产品活性：Oprozomib (PR-047) 是一种有效的，具有口服活性的选择性肽环氧酮类蛋白酶体 (proteasome) 抑制剂，对蛋白酶体 (β5) 和免疫蛋白酶体 (LMP7) 的 IC₅₀ 分别为 36 和 82 nM。 Oprozomib (ONX 0912) 诱导多发性骨髓瘤细胞凋亡 (apoptosis)。

研究领域：Metabolic Enzyme/Protease  |  Autophagy  |  Apoptosis

作用靶点：Proteasome  |  Autophagy  |  Apoptosis

In Vitro: 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.

In Vivo: 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.

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