货号	规格	价格	上海	北京	武汉	南京
S81123-1mg	99.6%	￥210.00 S81123-1mg ￥210.00 现货	6 6	-	-	-
S81123-2mg	99.6%	￥380.00 S81123-2mg ￥380.00 现货	5 5	-	-	-
S81123-5mg	99.6%	￥605.00 S81123-5mg ￥605.00 现货	6 6	-	-	-
S81123-10mg	99.6%	￥660.00 S81123-10mg ￥660.00 现货	4 4	-	-	-
S81123-25mg	99.6%	￥1490.00 S81123-25mg ￥1490.00 现货	4 4	-	-	-
S81123-50mg	≥99%	￥2650.00 S81123-50mg ￥2650.00 2-3天	0 货期：2-3天	-	-	-
S81123-100mg	≥99%	￥4200.00 S81123-100mg ￥4200.00 2-3天	0 货期：2-3天	-	-	-

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产品介绍

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

产品描述：

靶点：

Proteasome；Autophagy；Apoptosis;Proteasome; Autophagy

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.

参考文献：

1. Han-Jie Zhou, et al. Design and synthesis of an orally bioavailable and selective peptide epoxyketone proteasome inhibitor (PR-047). J Med Chem. 2009 May 14;52(9):3028-38. 2. Dharminder Chauhan,et al. A novel orally active proteasome inhibitor ONX 0912 triggers in vitro and in vivo cytotoxicity in multiple myeloma. Blood. 2010 Dec 2;116(23):4906-15. 3. M A Hurchla, et al.The epoxyketone-based proteasome inhibitors carfilzomib and orally bioavailable oprozomib have anti-resorptive and bone-anabolic activity in addition to anti-myeloma effects. Leukemia. 2013 Feb;27(2):430-40.

溶解性：

DMSO : ≥ 50 mg/mL (93.88 mM)

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.878 ml	9.388 ml	18.775 ml
5 mM	0.376 ml	1.878 ml	3.755 ml
10 mM	0.188 ml	0.939 ml	1.878 ml
50 mM	0.038 ml	0.188 ml	0.376 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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