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CEP-18770 (Delanzomib),蛋白酶体抑制剂

CEP-18770 (Delanzomib) （订货以英文为准）

编号：D127401
CAS号：847499-27-8
分子式：C21H28BN3O5
分子量：413.28
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D127401-5mg 阿拉丁 5mg ¥133.90
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D127401-25mg 阿拉丁 25mg ¥411.90
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D127401-10mg 阿拉丁 10mg ¥216.90
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D127401-100mg 阿拉丁 100mg ¥1329.90
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D127401-50mg 阿拉丁 50mg ¥664.90
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产品名称 CEP-18770 (Delanzomib)
中文名称 CEP-18770 (Delanzomib),蛋白酶体抑制剂
CAS号 847499-27-8
分子式（M.F.） C21H28BN3O5
分子量（M.W.） 413.28
储存条件 -20°C储存;充氩
溶解性DMSO 83 mg/mL Water <1 mg/mL Ethanol 83 mg/mL
存贮条件储存温度-20°C
备注CEP-18770 is an orally active inhibitor of the chymotrypsin-like activity of proteasome with IC50 of 3.8 nM, with only marginal inhibition of the tryptic and peptidylglutamyl activities of the proteosome. Phase 1/2.
生化机理Description:IC50 Value: 3.8 nM [1]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 and the expression of several NF-kappaB downstream effectors.in 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
别名(R)-1-((2S,3R)-3-hydroxy-2-(2-phenylpicolinamido)butanamido)-3-methylbutan-2-ylboronic acid;(R)-1-((2S,3R)-3-hydroxy-2-(2-phenylpicolinamido)butanamido)-3-methylbutan-2-ylboronic acid
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