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CEP-18770 (Delanzomib)

CAS number:847499-27-8    molecular formula:C21H28BN3O5

overview

compound 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。

Specs

Chinese aliasCEP-18770(德兰佐米)
English aliasDelanzomib, 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 number847499-27-8molecular formulaC21H28BN3O5
molecular weight413.28 g/molExact mass10mM in DMSO
PSA132.000 Ųlogp-

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