产品名称

英文名称：Carfilzomib

同义词

Carfilzomib、868540-17-4、Kyprolis、Carfilzomib (PR-171)、PR-171、UNII-72X6E3J5AR、Carfilzomib (PR171)、NSC-758252、72X6E3J5AR、DTXSID4048690、CHEBI65347、CHEMBL451887、DTXCID0028616、NSC 758252、NCGC00249613-01、(2S)-N-((1S)-1-Benzyl-2-(((1S)-3-methyl-1-(((2R)-2-methy、卡非佐米、Proteasomel抑制剂

产品性质

CAS编号：868540-17-4

分子式：C40H57N5O7

分子量：719.91

PubChem编号：11556711

别名：卡非佐米|Proteasomel抑制剂

英文别名：Carfilzomib|868540-17-4|Kyprolis|Carfilzomib (PR-171)|PR-171|UNII-72X6E3J5AR|Carfilzomib (PR171)|NSC-758252|72X6E3J5AR|DTXSID4048690|CHEBI65347|CHEMBL451887|DTXCID0028616|NSC 758252|NCGC00249613-01|(2S)-N-((1S)-1-Benzyl-2-(((1S)-3-methyl-1-(((2R)-2-methy

规格或纯度：≥99%

英文名称：Carfilzomib

生化机理：Carfilzomib, an irreversible proteasome inhibitor, has a favorable safety profile and significant anti-tumor activity in patients with relapsed and refractory multiple myeloma (MM). Here we summarize the clinical pharmacokinetics (PK), metabolism, and drμg-drμg interaction (DDI) profile of carfilzomib. The PK of carfilzomib, infused over 2-10 min, was evaluated in patients with solid tumors or MM. The proteasome has emerged as an important target for cancer therapy with the approval of bortezomib, a first-in-class, reversible proteasome inhibitor, for relapsed/refractory multiple myeloma (MM). Carfilzomib induced a dose- and time-dependent inhibition of proliferation, ultimately leading to apoptosis. Carfilzomib showed increased efficacy compared with bortezomib and was active against bortezomib-resistant MM cell lines and samples from patients with clinical bortezomib resistance. Carfilzomib has entered in a Phase II clinical trial in the treatment of multiple myeloma

储存温度：-20°C储存

运输条件：超低温冰袋运输

备注：如果有可能，您尽量在使用的当天配置溶液，并在当天使用完它。但是，如果您需要预先配制储备溶液，我们建议您将溶液等份保存在-20°C的密封小瓶中。通常，它们最多可以使用一个月。在使用前和打开样品瓶之前，我们建议您让您的产品在室温下平衡至少1小时。需要更多关于溶解度，用法和处理的建议吗？请访问我们的常见问题（FAQ）页面以获取更多详细信息。

产品介绍：Carfilzomib (PR-171)是一种不可逆proteasome抑制剂，IC50为<5 nM，在体外优先抑制β5亚基的ChT-L活性，对PGPH和T-L活性很弱或没有作用。Proteasomel抑制剂,epoxomicin的类似物Carfilzomib (PR-171) is an irreversible proteasome inhibitor with IC50 of <5 nM, displayed preferential in vitro inhibitory potency against the ChT-L activity in the β5 subunit, but little or no effect on the PGPH and T-L activities.Proteasome inhibitor, analog of epoxomicin

ALogP：4.7

IUPAC Name：(2S)-4-methyl-N-[(2S)-1-[[(2S)-4-methyl-1-[(2R)-2-methyloxiran-2-yl]-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]-2-[[(2S)-2-[(2-morpholin-4-ylacetyl)amino]-4-phenylbutanoyl]amino]pentanamide

INCHI：InChI=1S/C40H57N5O7/c1-27(2)22-32(36(47)40(5)26-52-40)42-39(50)34(24-30-14-10-7-11-15-30)44-38(49)33(23-28(3)4)43-37(48)31(17-16-29-12-8-6-9-13-29)41-35(46)25-45-18-20-51-21-19-45/h6-15,27-28,31-34H,16-26H2,1-5H3,(H,41,46)(H,42,50)(H,43,48)(H,44,49)/t31-,32-,33-,34-,40+/m0/s1

InChi Key：BLMPQMFVWMYDKT-NZTKNTHTSA-N

Canonical SMILES：CC(C)CC(C(=O)C1(CO1)C)NC(=O)C(CC2=CC=CC=C2)NC(=O)C(CC(C)C)NC(=O)C(CCC3=CC=CC=C3)NC(=O)CN4CCOCC4

Isomeric SMILES：CC(C)C[C@@H](C(=O)[C@]1(CO1)C)NC(=O)[C@H](CC2=CC=CC=C2)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC3=CC=CC=C3)NC(=O)CN4CCOCC4

PubChem CID：11556711

CAS Registry No.：868540-17-4

DrugBank Ligand：DB08889

ChEMBL Ligand：CHEMBL451887

Wikipedia：Carfilzomib

DrugCentral Ligand：4483

溶解性：DMSO 50 mg/mL Water <1 mg/mL Ethanol <1 mg/mL

象形图：

信号词：Danger

危险声明：H315 Causes skin irritationH319 Causes serious eye irritationH335 May cause respiratory irritationH413 May cause long lasting harmful effects to aquatic lifeH302 Harmful if swallowedH300 Fatal if swallowedH372 Causes damage to organs through prolonged or repeated exposureH361 Suspected of damaging fertility or the unborn child

预防措施声明：P261,P305+P351+P338,P273,P280,P302+P352,P321,P405,P501,P264,P260,P271,P270,P304+P340,P403+P233,P362+P364,P330,P203,P264+P265,P301+P316,P301+P317,P318,P337+P317,P332+P317,P319

产品包装