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CEP-18770(Delanzomib)

更新时间:2025-08-30 20:10:17 采购访问:105次

常用名 Delanzomib CAS号 847499-27-8
价格 纯度 98.0%
备货期 10天 库存 现货
 产品详情(用途,包装等)
用途:
Delanzomib(CEP-18770) is a novel orally-active inhibitor of the chymotrypsin-like activity of the proteasome that down-modulates the nuclear factor-kappaB (NF-kappaB) activity.IC50 Value: 3.8 nM [1]Target: proteasomein vitro: CEP-18770 and bortezomib showed comparable potency against chymotrypsin-like proteasome activity, cellular inhibitory activity (IC50) values of 3.8 (± 1.0) nM and 3.8 (± 0.4) nM, respectively, CEP-18770 had a 2- to 11-fold lower cytotoxic potency compared with bortezomib against solid tumor cell lines, comparable potency against 2 hematologic tumor cell lines, and a similar spectrum of antiproliferative activity with IC50 values for both compounds of less than 35 nM [1].in vivo: in MM xenograft models, the addition of CEP-18770 IV to melphalan completely prevented the growth of both melphalan-sensitive and melphalan-resistant tumours. The combination of CEP-18770 IV and bortezomib induced complete regression of bortezomib-sensitive tumours and markedly delayed progression of bortezomib-resistant tumours compared to treatment with either agent alone [2]. Age matched MRL/lpr or NZBWF1 mice with established SLE or LN, respectively, were treated with delanzomib either 3 mg/kg once or twice weekly intravenously or orally at 10 mg/kg [3]. Toxicity: CEP-18770 showed a favourable safety profile with lack of neurotoxicity and linear plasma PK. The definition of the optimal biological dose and schedule of treatment is actively pursued because of the high incidence of skin toxicity of the twice a week schedule [4].Clinical trial: CEP-18770 in Combination With Lenalidomide and Dexamethasone in Relapsed or Refractory Multiple Myeloma. Phase1/2
物理化学性质:
CAS号:847499-27-8
常用中文名:Delanzomib
常用英文名:CEP-18770 (Delanzomib)
分子式:C21H28BN3O5
分子量:413.275
密度:1.207
沸点:N/A
熔点:N/A
闪点:N/A
储存条件:-20℃

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上海化源世纪贸易有限公司 认证供应商

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参考价格:$165/10mM*1mLinDMSO