卡非佐米

强大的不可逆蛋白酶体抑制剂

规格或纯度: ≥99%

CAS编号: 868540-17-4
分子式: C₄₀H₅₇N₅O₇
分子量: 719.91
PubChem编号: 11556711

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货号 (SKU)	包装规格	是否现货
C127870-5mg	5mg	现货
C127870-10mg	10mg	现货
C127870-25mg	25mg	现货
C127870-50mg	50mg	现货
C127870-100mg	100mg	现货
C127870-500mg	500mg	现货

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proteasome 20S subunit beta 5 Inhibitor

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基本描述

规格或纯度	≥99%
英文名称	Carfilzomib
别名	卡非佐米;Proteasomel抑制剂
英文别名	PR 171;PR171;PR-171; (alphaS)-alpha-[(4-Morpholinylacetyl)amino]benzenebutanoyl-L-leucyl-N-[(1S)-3-methyl-1-[[(2R)-2-methyloxiranyl]carbonyl]butyl]-L-phenylalaninamide
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

名称和标识符

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
分子式	C₄₀H₅₇N₅O₇
PubChem CID	11556711
分子量	719.91

数据库链接

PubChem CID	11556711
CAS Registry No.	868540-17-4
DrugBank Ligand	DB08889
ChEMBL Ligand	CHEMBL451887
Wikipedia	Carfilzomib
DrugCentral Ligand	4483

化学和物理性质

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

安全信息

象形图	Toxic Health Hazard Harmful
信号词	Danger
危险声明	H315: Causes skin irritation H319: Causes serious eye irritation H335: May cause respiratory irritation H413: May cause long lasting harmful effects to aquatic life H302: Harmful if swallowed H300: Fatal if swallowed H372: Causes damage to organs through prolonged or repeated exposure H361: 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

靶标

Target ID

2406

名称

proteasome 20S subunit beta 5

缩写名

SHP2

家族

T1: Proteasome

别名

food intake receptor

基因和蛋白信息

Species	Transmembrane Domains	Amino Acids	Chromosomal Location	Gene Symbol	Gene Name
Human	2	263	14q11.2	PSMB5	proteasome 20S subunit beta 5
Mouse	2	264	14 27.86 cM	Psmb5	proteasome (prosome, macropain) subunit, beta type 5
Rat	2	263	15p13	Psmb5	proteasome 20S subunit beta 5

OMIM

600306 (Hs)

Entrez Gene

5693 (Hs) , 19173 (Mm) , 29425 (Rn)

UniProtKB

P28074 (Hs) , O55234 (Mm) , P28075 (Rn)

RefSeq Protein

NP_001124197 (Hs) , NP_001138404 (Hs) , NP_002788 (Hs) , NP_035316 (Mm) , NP_001099197 (Rn)

RefSeq Nucleotide

NM_001130725 (Hs) , NM_001144932 (Hs) , NM_002797 (Hs) , NM_011186 (Mm) , NM_001105727 (Rn)

Ensembl Gene

ENSG00000100804 (Hs) , ENSMUSG00000022193 (Mm) , ENSRNOG00000013386 (Rn)

MEROPS

T01.P01 (Hs)

Protein GI

195539356 (Hs) , 222144262 (Hs) , 4506201 (Hs) , 6755204 (Mm) , 160333293 (Rn)

DrugBank Target

P28074 (Hs)

CATH/Gene3D

3.60.20.10 (N/A)

ChEMBL Target

CHEMBL4662 (Hs) , CHEMBL4523208 (Rn) , CHEMBL1944494 (Mm)

关联配体

Ligand ID	7420
名称	carfilzomib
别名	PR-171
类别	Synthetic organic
学名	(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
生物活性评价	Carfilzomib causes a dose-dependent inhibition of 20S proteasomal chymotrypsin-like activity in CD138⁺ plasma cells purified from MM patient samples . Maximum inhibition of approximately 70% is achieved with 10-25nM carfilzomib.
评价	Carfilzomib is a tetrapeptide analogue of epoxomicin, an Actinomycete derived selective proteasome inhibitor .

参考文献

1. Hanada M, Sugawara K, Kaneta K, Toda S, Nishiyama Y, Tomita K, Yamamoto H, Konishi M, Oki T. (1992) Epoxomicin, a new antitumor agent of microbial origin.. J Antibiot, 45 (11): (1746-52). [PMID:1468981]
2. Kuhn DJ, Chen Q, Voorhees PM, Strader JS, Shenk KD, Sun CM, Demo SD, Bennett MK, van Leeuwen FW, Chanan-Khan AA et al.. (2007) Potent activity of carfilzomib, a novel, irreversible inhibitor of the ubiquitin-proteasome pathway, against preclinical models of multiple myeloma.. Blood, 110 (9): (3281-90). [PMID:17591945]
3. Wang ES et al.. (2021) Acute pharmacological degradation of Helios destabilizes regulatory T cells.. Nat Chem Biol, 17 (6): (711-717). [PMID:34035522]

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卡非佐米

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卡非佐米

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基本描述

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化学和物理性质

安全信息

靶标

关联配体

参考文献

相关文档

质检报告COA

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