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Product introduction

Delanzomib (CEP-18770)是一种具有胰凝乳蛋白酶样活性的蛋白酶体抑制剂，IC50为3.8 nM，只最低限度地抑制蛋白酶体的胰蛋白酶和肽谷氨酰基活性。 CEP-18770是一种新型的、有效的和可逆的P2苏氨酸硼酸类蛋白酶体抑制剂，通过下调核因子-κB（NF-κB）的活性及其几个下游效应子的表达，从而抑制蛋白酶体的糜蛋白酶样活性，IC50值为3.8 nM。多项研究的初步结果表明：在人多发性骨髓瘤（MM）细胞系中，CEP-18770通过诱导细胞凋亡，发挥有效的抗肿瘤活性；通过抑制RANKL诱导的破骨细胞生成，具有强烈的抗血管生成活性；对正常细胞具有较轻的毒性反应，包括上皮细胞、骨髓祖细胞和骨髓衍生的基质细胞。

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Chinese name

CEP-18770 (Delanzomib)

English name

CEP-18770 (Delanzomib)

Chinese alias

CEP-18770(德兰佐米)

English alias

Delanzomib, free base | NCGC00346469-01 | NPH007098 | NPH-007098 | DTXSID901025656 | CEP18770 | CEP-18770 | Cilostamide, phosphodiesterase inhibitor | [(1R)-1-[[(2S,3R)-3-hydroxy-2-[(6-phenylpyridin-2-yl)carbonylamino]butanoyl]amino]-3-methyl-butyl]boroni

CAS number

847499-27-8

molecular formula

C21H28BN3O5

molecular weight

413.28 g/mol

Exact mass

10mM in DMSO

PSA

132.000 Å²

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