Carfilzomib (PR-171)

For research use only. Not for use in humans.

目录号：S2853 中文名称：卡非佐米

CAS No. 868540-17-4

Carfilzomib (PR-171) 是一种不可逆proteasome抑制剂，在ANBL-6细胞中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。Carfilzomib 可激活自噬并诱导细胞凋亡。

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购买数量

10mM (1mL in DMSO)	RMB 3898.94	现货
5mg	RMB 1377.06	现货
10mg	RMB 2211.31	现货
50mg	RMB 5500.54	现货
100mg	RMB 7125.64	现货
200mg	RMB 9582.3	现货
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客户使用Selleck生产的Carfilzomib (PR-171)发表文献140篇：

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Cell, 2019, 36(2):179-193

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Mol Cancer Ther, 2021, 20(2):367-378

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Nat Commun, 2020, 22;11(1):1931

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Autophagy, 2020, 10.1080/15548627.2020.1740529

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Oncogene, 2020, 9

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Cell Mol Life Sci, 2020, 10.1007/s00018-020-03568-x

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Front Immunol, 2020,

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Cancer Sci, 2020, 111(4):1279-1290

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Acta Pharmacol Sin, 2020, 10.1038/s41401-020-00544-w

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Clin Cancer Res, 2020, clincanres.1232.2020

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Blood Adv, 2020, 4(18):4312-4326

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Autophagy, 2020, 1-13

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Nat Chem Biol, 2020, 10.1038/s41589-020-0594-x

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Br J Cancer, 2020, 10.1038/s41416-020-01191-y

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Neurooncol Adv, 2020, 2(1):vdaa051

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Oncotarget, 2020, 11(44):3984-3997

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Cell Rep, 2020, 32(2):107897

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J Zhejiang Univ Sci B, 2020, 21(1):64-76

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Mol Cell, 2019, 75(4):849-858

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Nat Chem Biol, 2019, 15(3):232-240

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EMBO Mol Med, 2019, 11(10):e9930

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Leukemia, 2019, 10.1038/s41375-019-0525-6

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Cell Rep, 2019, 28(12):3224-3237

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Cancers (Basel), 2019, 11(7)

PubMed: 31315220 ( click the link to review the publication )

PLoS Pathog, 2019, 15(1):e1007498

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Cell Death Dis, 2019, 10(8):611

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Arch Toxicol, 2019, 93(4):953-964

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Cell Chem Biol, 2019, 10.1016/j.chembiol.2019.10.013

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Cell Chem Biol, 2019, 26(3):340-351

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Cell Physiol Biochem, 2019, 53(6):999-1014

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Mol Cancer Ther, 2019, 18(11):2097-2110

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Biochim Biophys Acta Mol Basis Dis, 2019, 1865(6):1666-1676

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Amyloid, 2019, 26(1):24-33

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Mol Cancer Res, 2019, 10.1158/1541-7786

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Int J Mol Sci, 2019, 20(24)

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Sci Rep, 2019, 9(1):18409

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Sci Rep, 2019, 9(1):18062

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Apoptosis, 2019, 24(5-6):404-413

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Biochem J, 2019, 476(21):3211-3226

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PLoS One, 2019, 14(12):e0225727

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J Hematol Oncol, 2018, 11(1):112

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Cancer Lett, 2018,

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Cell Death Dis, 2018, 9(2):162

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Mol Cancer Ther, 2018, 17(12):2610-2621

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Hum Mol Genet, 2018, 27(3):451-462

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Ann Hematol, 2018, 97(5):839-849

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SLAS Discov, 2018, 23(5):459-473

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Oncotarget, 2018,

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Oncotarget, 2018, 9(29):20265-20281

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FEBS J, 2018, 285(3):467-480

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Blood, 2017, 5;129(1):88-99

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Nat Commun, 2017, 8:14290

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Clin Cancer Res, 2017, 23(16):4817-4830

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Exp Mol Med, 2017, 49(8):e365

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Mol Cancer Ther, 2017, 16(11):2375-2386

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Sci Rep, 2017, 7(1):8027

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J Pharmacol Exp Ther, 2017, 363(1):20-34

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PLoS One, 2017, 12(2):e0173013

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Leuk Lymphoma, 2017, 58(12):2916-2925

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Cancer Metab, 2017, 5:7

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Cell Host Microbe, 2017, 22(4):507-518

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Nat Cell Biol, 2016, 18(8):897-909

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EMBO J, 2016, 35(23):2602-2613

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Leukemia, 2016, 30(1):104-11

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Proc Natl Acad Sci U S A, 2016, 113(46):13162-13167

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Matrix Biol, 2016, 55:22-34

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Cardiovasc Res, 2016, 110(2):188-99

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PLoS Pathog, 2016, 12(10):e1005929

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PLoS Genet, 2016, 12(9):e1006279

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Bioinformatics, 2016, 32(12):i253-i261

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Leuk Lymphoma, 2016, 57(7):1677-86

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Horm Cancer, 2016, 7(5-6):345-355

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Oncotarget, 2016, 7(25):38523-38538

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Oncotarget, 2016, 7(4):4454-67

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Oncotarget, 2016, 7(2):1598-607

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Blood, 2015, 125(2):407-10

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Leukemia, 2015, 29(6):1390-401

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PLoS One, 2015, 10(3):e0119546

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Chem Biol, 2015, 22(6):755-63

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Oncotarget, 2015, 6(19):17532-42

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Chem Biol, 2015, 10.1016/j.chembiol.2015.01.004

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产品安全说明书

Proteasome抑制剂选择性比较

生物活性

产品描述

靶点

Proteasome ^[1]
(ANBL-6 cells)

5 nM

体外研究

Carfilzomib抑制多种细胞系和源自患者的肿瘤细胞的增殖，包括多发性骨髓瘤。Carfilzomib诱导内在和外在的凋亡信号传导途径并激活c-Jun N-末端激酶(JNK)。与bortezomib相比，Carfilzomib协同地塞米松(Dex)表现增强的抗MM活性，并克服了bortezomib等药物的抗性。 Carfilzomib有选择地抑制β5亚基的CHT- L活性，在10 nM剂量时抑制超过80％的活性。低剂量Carfilzomib短期处理导致优先结合特异性的β5组成20S蛋白酶体和β5i免疫蛋白酶体亚基。在Carfilzomib刺激的ANBL -6细胞中检测caspase活性，结果显示caspase- 8和caspase -9和caspase-3活性在8小时后大幅增加，和对照8小时后的细胞相比分别增加了3.2 ， 3.9和6.9倍。在carfilzomib处理过的细胞中，线粒体膜的完整性减少到41%(Q1 + Q2)，而在对照细胞中这一比例为75％。^[1] 在另一项研究中，Carfilzomib也表现出对血液和实体肿瘤的临床前有效性。^[2] Carfilzomib直接一直破骨形成和骨吸收。^[3]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
MM.1S	MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NIHXfWsxNTFyMDDuUS=>	MWO0PEBp	NX\ERVhoUUN3MNMgQeKhOTBibl2=	NWm5bFc4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzNVI2PDNpPkK1N\|EzPTR\|PD;hQi=>
NCI-H929	Mn3XS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MYOwMVExOCCwTR?=	Mn\YOFghcA>?	Ml;ITWM2OCB;wrCxOEBvVQ>?	NIHlU4c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUOxNlU1Oyd-MkWzNVI2PDN:L3G+
SUDHL16	MYTBdI9xfG:\|aYOgRZN{e2G7	M{fWRVIvPeLCk{OuOUBvVQ>?	NGi4[Vk1QCCq	Mnjx[Y5p[W6lZYOgeIhmKGOnbHyg[IVifGhiY3:teJJm[XSvZX70JJdqfGhiQVPZNVIyPQ>?	M2fZ[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkO5PVM2Lz5{NUKzPVk{PTxxYU6=
SUDHL14	MWPBdI9xfG:\|aYOgRZN{e2G7	MYKyMlXjiJN\|LkWgcm0>	NWHUdFY{PDhiaB?=	NWjUTpdt\W6qYX7j[ZMhfGinIHPlcIwh\GWjdHigZ48ufHKnYYTt[Y51KHerdHigRWN[OTJzNR?=	MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJ\|OUmzOUc,OjV{M{m5N\|U9N2F-
U2932	M3zUfWFxd3C2b4Ppd{BCe3O\|YYm=	MkDPNk426oDVMz61JI5O	M3TYd\|Q5KGh?	MXvlcohidmOnczD0bIUh[2WubDDk[YF1cCClbz30doVifG2nboSge4l1cCCDQ2mxNlE2	NFjjOYE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUKzPVk{PSd-MkWyN\|k6OzV:L3G+
P-UMSCC-1	MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?			NXHXOoJ{UUN3ME2xNU4zKG6P	Mn3FQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MUWwN\|koRjJ2OUG1NFM6RC:jPh?=
R-UMSCC-1	M{fIbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7			MXzJR\|UxRTJ{OUSgcm0>	M4LvN\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUG1NFM6Lz5{NEmxOVA{QTxxYU6=
P-Cal33	NVLme3BsT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=			NUPKNY5mUUN3ME2xO{4{KG6P	MlnLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MUWwN\|koRjJ2OUG1NFM6RC:jPh?=
R-Cal33	MkLQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?			MmLqTWM2OD1zMUGyJI5O	MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlzNUCzPUc,OjR7MUWwN\|k9N2F-
Jurkat	MkTtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NW\Lcm9COS1zMX7N	M4nIXVQ5KGh?	NV72NVUxcW6qaXLpeJMhfGinIHPlcIwheHKxbHnm[ZJifGmxbjDjc{11emWjdH3lcpQhf2m2aDD2c5Jqdm:\|dHH0	MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDhyMUGyPEc,OjR6MEGxNlg9N2F-
Jurkat	NHLh[WJCeG:ydH;zbZMhSXO\|c3H5	MXO4JI5O	MkHxNlQwPDhiaB?=	MlnhbY5lfWOnczDhdI9xfG:\|aYOsJINie3Cjc3WgZYN1cX[jdHnvckwh[W6mIGDBVnAh[2ynYY\h[4Uh[29vdILlZZRu\W62IIfpeIghfm:{aX7vd5RifA>?	NEDBbJo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEiwNVEzQCd-MkS4NFEyOjh:L3G+
UMSCC-22A	NUfhVYNCSXCxcITvd4l{KEG\|c4PhfS=>	MWCyNFAhdk1?	MnGyNlQhcA>?	MYDpcoR2[2VidHjlJINmdGxiYYDvdJRwe2m\|IHPvMZRz\WG2bXXueEB4cXSqIF;OXEAxQTF{	M2W1NFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{OUK5PFA{Lz5{MkmyPVgxOzxxYU6=
UMSCC-22B	MYnBdI9xfG:\|aYOgRZN{e2G7	MU[yNFAhdk1?	M4LqPVI1KGh?	NEDjcG5qdmS3Y3WgeIhmKGOnbHygZZBweHSxc3nzJINwNXS{ZXH0cYVvfCC5aYToJG9PYCByOUGy	NYnLcHluRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK5Nlk5ODNpPkKyPVI6QDB\|PD;hQi=>
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UMSCC-1	MYrBdI9xfG:\|aYOgRZN{e2G7	NE\1XWozODBibl2=	MmPONlQhcA>?	NHLmT2xqdmS3Y3WgeIhmKGOnbHygZZBweHSxc3nzJINwNXS{ZXH0cYVvfCC5aYToJG9PYCByOUGy	Mn;2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ7Mkm4NFMoRjJ{OUK5PFA{RC:jPh?=
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RPMI8226	MUnDfZRwfG:6aXPpeJkh[XO\|YYm=		MlLUO\|IhcHK\|	MUfDfZRwfG:6aXOgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCUUF3JPFIzPiClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRUKGG\|c3H5MEBKSzVyIE2gNE4xOTNzOTFOwG0v	MnvFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR5Nke4NVgoRjJ2N{[3PFE5RC:jPh?=
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RPMI8266	NF\PeJhCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=		MkHjO\|IhcHK\|	MYLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFKSTVm4NlY3KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDvfJltfWOrZnXybY4hdHWvaX7ld4NmdmOnIHHzd4F6NCCLQ{WwJF0hOC5yMUO5JO69VS5?	NY\DNpM6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[yN\|EyPjJpPkK2NlMyOTZ{PD;hQi=>
HCT116	MoXRRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?		NFT5Sow4OiCqcoO=	NX\rdYtRSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[W[2ZYKgO\|IhcHK\|IHL5JI95gWy3Y3nm[ZJqdiCudX3pcoV{[2WwY3WgZZN{[XluIFnDOVAhRSByLkCxPVMh\|ryPLh?=	NIjCcGU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkKzNVE3Oid-Mk[yN\|EyPjJ:L3G+
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A673	MV7xTHRUKGG\|c3H5			MWnxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDBOlc{KGOnbHzzLS=>	NFPCSo09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
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BT-37	MW\xTHRUKGG\|c3H5			MYTxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDCWE0{PyClZXzsdy=>	MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
MG 63 (6-TG R)	MlfudWhVWyCjc4PhfS=>			NETKN2RyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBOTyB4MzCoOk1VTyCUKTDj[Yxtew>?	M2n4[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Rh30	NF3RTJlyUFSVIHHzd4F6			NHfrUXRyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBTcDNyIHPlcIx{	M1j2bVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
fibroblast cells	NUTmNoJGeUiWUzDhd5NigQ>?			MmqwdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgZ49vfHKxbDDIbEB4cWymIIT5dIUh\mmkcn;icIF{fCClZXzsdy=>	MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
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TC32	NUP1bZJjeUiWUzDhd5NigQ>?			NXnVcGhVeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiT4L0bI9od26jbDCzSEBk[XOyYYPlJJNkemWnbjDmc5IhXEN\|MjDj[Yxtew>?	MmrKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
TC32	MoTKdWhVWyCjc4PhfS=>			MoDKdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohV3K2aH;nc45idCB\|RDD2bYFjcWyrdImgd4Nz\WWwIH\vdkBVSzN{IHPlcIx{	NX75bpZCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
MG 63 (6-TG R)	Ml7vdWhVWyCjc4PhfS=>			MXjxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBQenSqb3fvcoFtKDOGII\pZYJqdGm2eTDzZ5Jm\W5iZn;yJG1IKDZ\|IDi2MXRIKFJrIHPlcIx{	MnvTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
SJ-GBM2	M3\qcZFJXFNiYYPzZZk>			MVfxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0pvR1LNNkBk\Wyucx?=	MoDvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
SK-N-MC	Mn\ldWhVWyCjc4PhfS=>			M2LrVJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSz3OMW1EKGOnbHzz	M2HyUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
NB-EBc1	MlfDdWhVWyCjc4PhfS=>			MUPxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVkJvRVLjNUBk\Wyucx?=	NEfkN\|Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
LAN-5	MojQdWhVWyCjc4PhfS=>			NGXUTGRyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTFHOMVUh[2WubIO=	M4fXeVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Rh18	NUDzelhqeUiWUzDhd5NigQ>?			MlzWdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKqMUigZ4VtdHN?	M3TWZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SK-N-MC	MkjNdWhVWyCjc4PhfS=>			NInaNGhyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBUUy2QLV3DJINmdGy\|	MkT1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
SJ-GBM2	MmO1dWhVWyCjc4PhfS=>			NYPpb\|dteUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhW0pvR1LNNkBk\Wyucx?=	NGS1[5o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
TC32	M3zTd5FJXFNiYYPzZZk>			Mom2dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgWGM{OiClZXzsdy=>	MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
Rh18	M3GzfJFJXFNiYYPzZZk>			NFnuOZFyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBTcDF6IHPlcIx{	Mn;CQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
Saos-2	M33NPJFJXFNiYYPzZZk>			NEf3NodyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBU[W:\|LUKgZ4VtdHN?	MnTVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
SJ-GBM2	MmXSdWhVWyCjc4PhfS=>			NH\V[phyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCRcoToc4dwdmGuIEPEJJZq[WKrbHn0fUB{[3KnZX6g[o9zKFOMLVfCUVIh[2WubIO=	MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
RD	M{HEdZFJXFNiYYPzZZk>			NWTGUIV3eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiT4L0bI9od26jbDCzSEB3cWGkaXzpeJkhe2O{ZXXuJIZweiCURDDj[Yxtew>?	MlPKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
ANBL-6	NEDWcnJHfW6ldHnvckBie3OjeR?=			NHH3NXVKdmirYnn0bY9vKG:oIEKwV{Bxem:2ZXHzc41mKGGldHn2bZR6KGmwIHj1cYFvKEGQQlytOkBk\WyuczygTWM2OCB;IECuNFEh\|ryPLh?=	NF:xXGs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OU[1NlE1Oyd-Mkm2OVIyPDN:L3G+
MCF7	NUXERY17S3m2b4TvfIlkcXS7IHHzd4F6		M3fW[VQ5KGi{cx?=	NWDp[5A5S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUOINzDj[YxteyCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwJF0hOC5yMESxJO69VS5?	MnvsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzBzNkWzOFQoRjNyMU[1N\|Q1RC:jPh?=
MDA-MB-231	Mkf6R5l1d3SxeHnjbZR6KGG\|c3H5		NYnCWpNFPDhiaILz	MoTER5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUKzNUBk\WyuczDh[pRmeiB2ODDodpMh[nliTWTUJIF{e2G7LDDJR\|UxKD1iMD6wNFQ1KM7:TT6=	NIHQbYI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9\|MEG2OVM1PCd-M{CxOlU{PDR:L3G+
RPMI8226	Mn\xR5l1d3SxeHnjbZR6KGG\|c3H5		MVG0PEBpenN?	NYXGNpo6S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hWlCPSUiyNlYh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygTWM2OCB;IECuNFA3PyEQvF2u	NFzyNWU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9\|MEG2OVM1PCd-M{CxOlU{PDR:L3G+

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	pERK / ERK / pSTAT5 / STAT5 / pPI3K / PI3K; PubMed: 24590311 Oncogenesis Western blot analysis for activated (phosphorylated) ERK, Stat5 and PI3K signaling pathways following exposure to carfilzomib, total levels of ERK, Stat5 and PI3K were used as a loading control. caspase-9 / caspase-8; PubMed: 24590311 Oncogenesis Western blot analysis for activated (cleaved) caspase-8 and caspase-9 following exposure to carfilzomib. c-PARP / PARP / caspase-3; PubMed: 22929803 Clin Cancer Res UMSCC-22A, UMSCC-22B, 1483 and UMSCC-1 cells were treated for 24 hours with 0.1% DMSO, or 200 nmol/L carfilzomib or ONX 0912, followed by immunoblotting with anti-PARP, anti-caspase-3, or anti-β-actin. Shown are full-length PARP, cleaved PARP (c-PARP), and the cleaved, active subunits of caspase-3. Similar results were obtained in 3 independent experiments. Bcl-2 / Bcl-Xl / Mcl-1 / Bik / Bim / Bax / Bak; PubMed: 22929803 Clin Cancer Res UMSCC-22A, UMSCC-22B, 1483 and UMSCC-1 cells were treated for 24 hours with 0.1% DMSO, or 100 nmol/L carfilzomib or ONX 0912, followed by immunoblotting for the indicated proteins. In the case of Bik immunoblotting, cells were treated with 200 nmol/L carfilzomib or ONX 0912 to more clearly demonstrate Bik upregulation in 1483 and UMSCC-1 cells. Blots shown are representative of 3 independent experiments. Atg5 / Atg12 / Beclin-1 / LC3-II; PubMed: 22929803 Clin Cancer Res HNSCC cells were treated for 24 hours with 100 nmol/L carfilzomib or ONX 0912, or with 0.1% DMSO. Immunoblots were probed for Beclin-1, Atg5/12 conjugate, LC3-II, or β-actin. Representative blots from 3 independent experiments are shown. Noxa / Bik / Puma / Mcl-1; PubMed: 25548100 Mol Cancer Res SW620 cells were treated with the indicated dosage for 48 h. Expression of Noxa, Bik and/or Puma, c-myc and Mcl-1 proteins was then analyzed by immunoblotting. Tubulin served as control for protein loading. EGFR / HER2 / ER alpha / p-Akt(Ser473) / Akt / p-ERK / ERK / p53; PubMed: 29069787 Oncotarget T47D and MCF7 cells were cultured with the indicated carfilzomib concentrations for 32 or 36 hours, respectively. Western blots of protein lysates were probed with the indicated antibodies. β-actin served as loading control. BDP1 / HER2(Tyr1248) / HER2(Tyr1221/Tyr1222) / PARP1 / caspase-7 / p53 Mut; PubMed: 29069787 Oncotarget BT474 cells were cultured in the presence of the indicated carfilzomib concentrations for 32 hours. Western blots of protein lysates were probed with the indicated antibodies. HLA class I; PubMed: 26323098 Oncotarget Immunofluorescence analysis was performed to confirm the consequence that down-regulation of HLA class I was in a dose- and time-dependent manner.	24590311 22929803 25548100 29069787 26323098
Growth inhibition assay	Cell viability; PubMed: 27655642 Oncotarget Cytotoxic effects of carfilzomib on breast cancer cells in MTT assays. Seven human breast cancer cell lines, MCF7, T-47D, MDA-MB-361, HCC1954, MDA-MB-468, MDA-MB-231, and BT-549 were treated with carfilzomib at 0, 0.001 μM, 0.01 μM, 0.05 μM, 0.1 μM, 1 μM, 10 μM, or 50 μM for 72 h, then subjected to MTT assays. The absorbance of each well was measured at 540 nm and plotted for the cell viability curve. IC50 values of carfilzomib in breast cancer cell lines were listed.	27655642

体内研究

Carfilzomib适度降低了体内异种移植物模型中肿瘤的生长。在持续或短暂处理下， Carfilzomib有效地降低多发性骨髓瘤细胞活力。 Carfilzomib增加骨小梁体积，减少骨吸收，并提高非肿瘤小鼠的骨形成。^[3]

激酶实验：^[1]	- 合并酶联免疫吸附试验分析carfilzomib亚基: ANBL -6细胞（2 ×10⁶/孔）接种于96孔板中并用Carfilzomib（0.001至10μM）处理 1小时。然后将细胞裂解（20mM的Tris-HCl， 0.5 mM EDTA），并裂解物上清转移到聚合酶链反应（PCR）平板上。使用起始浓度为6 μg/μL处理ANBL - 6细胞得到的裂解物做标准曲线。活性位点探针[生物素-(CH2)4-Leu-Leu-Leu-环氧酮; 20 μM]加入并于室温温育1小时。在细胞裂解液中添加1％十二烷基硫酸钠（SDS）和加热至100℃变性，随后在96孔的多屏DV板中每孔和20μL链霉亲和琼脂糖高性能珠混合并孵育1小时。这些珠粒用酶联免疫吸附试验(ELISA)缓冲液（PBS，1％牛血清白蛋白和0.1 ％吐温-20）洗涤细胞，并温育过夜，在4℃在板振荡器上与抗体的蛋白酶体亚基反应。所用抗体包括鼠单克隆抗- β1 ，抗-β2 ，抗β1i和抗β5i ，山羊多克隆抗β2i ，和兔多克隆抗- β5 （针对KLH- CWIRVSSDNVADLHDKYS肽亲和纯化的抗血清）。珠粒洗涤后用以辣根过氧化物酶标记的二羊抗兔，羊抗鼠或兔antigoat抗体温育2小时。洗涤后，将珠粒用SuperSignal ELISA picochemiluminescence底物反应，而后进行荧光检测。荧光信号通过与标准曲线比较转换为μg/mL，表示为抑制相对于对照的％。使用以下nonsigmoidal剂量 - 反应方程生成拟合曲线：Y = Bottom + (Top-Bottom)/(1 + 10̂((LogEC50 − X) × HillSlope))，其中X是浓度的对数， Y是抑制％，EC 50是表示50％的效果的剂量。
细胞实验：^[1]	- 合并 Cell lines: WST-1, ANBL-6细胞 Concentrations: 100 nM Incubation Time: 1小时 Method: WST-1被用于确定蛋白酶体抑制剂Carfilzomib对细胞增殖的影响。增殖的抑制作用是与对照细胞比较所得。线性样条函数是用来使用XLfit4软件进行计算半数抑制浓度（IC50）。抗性程度(DOR)的计算公式是IC50（抗性细胞）/ IC50（敏感细胞）。 ANBL-6细胞用100nM carfilzomib短暂处理，洗涤并悬浮于含有5μg/mL JC-1PBS中，它显示出在线粒体电位依赖性积聚。用FACScan分析线粒体膜电位依赖性颜色转变（从525到590 nM），数据用CellQuest软件分析。 (Only for Reference)
动物实验：^[4]	- 合并 Animal Models: Beige-nude-XID小鼠 Dosages: 2.0 mg/kg Administration: 静脉注射 (Only for Reference)

参考文献

[4] Dasmahapatra G, et al. Mol Cancer Ther. 2011, 10(9), 1686-1697.

- 合并

溶解度 (25°C)

体外	DMSO	50 mg/mL (69.45 mM)
	Water	Insoluble
	Ethanol	Insoluble
体内	从左到右依次将纯溶剂加入产品，现配现用(数据来自Selleck实验检测而非文献)： 2% DMSO+30% PEG 300+2%Tween 80+ddH2O	1mg/mL

* 溶解度检测是由Selleck技术部门检测的，可能会和文献中提供的溶解度有所差异，这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据 Download Carfilzomib (PR-171) SDF

分子量	719.91
化学式	C₄₀H₅₇N₅O₇
CAS号	868540-17-4
储存条件	3年-20°C 粉状 2年-80°C 溶于溶剂
别名	N/A

动物体内配方计算器 (澄清溶液)

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量

mg/kg

动物平均体重

每只动物给药体积

动物数量

只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO+ % + % Tween 80+ % ddH₂O

计算重置

计算结果:

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

质量

浓度

体积

分子量
=

×

×

*在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。

稀释计算器

用本工具协助配置特定浓度的溶液，使用的计算公式为：

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入输出 )

C1

V1

C2

V2
×

=

×

在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。.

连续稀释计算器方程

连续稀释
初始浓度:
稀释倍数:

计算结果

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

分子量计算器

通过输入化合物的化学式来计算其分子量：

注：化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×
计算

临床试验信息 (data from https://clinicaltrials.gov, updated on 2021-01-06)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04407858	Recruiting	--	Myeloma\|Heart Failure\|Hypertension	European Georges Pompidou Hospital	May 21 2020	--
NCT03673826	Recruiting	Drug: Carfilzomib\|Drug: Dexamethasone\|Drug: Lenalidomide	Smouldering Myeloma	Stichting Hemato-Oncologie voor Volwassenen Nederland	November 19 2018	Phase 2

技术支持

在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题，请给我们留言。

常见问题及建议解决方法

问题 1：
How should I prepare solution of Carfilzomib for ongoing in vivo study?
回答：
This compound can be dissolved in 2% DMSO/30% PEG 300/dd H2O at 10 mg/ml as a suspension, and can be dissolved in 2% DMSO/ castor oil at 10 mg/ml as a clear solution.

Proteasome Signaling Pathway Map

Proteasome Inhibitors with Unique Features

泛Proteasome抑制剂

Ixazomib (MLN2238) : β5 site, IC50=3.4 nM; β1 site, IC50=31 nM; β2 site, IC50=3500 nM.
活性最高的Proteasome抑制剂

Bortezomib (PS-341) : 20S proteasome, K_i of 0.6 nM.
最新的Proteasome抑制剂

Oprozomib (ONX 0912) : Orally bioavailable inhibitor for CT-L activity of 20S proteasome β5/LMP7 with IC50 of 36 nM/82 nM.
经典的Proteasome抑制剂

ONX-0914 (PR-957) : Selective immunoproteasome inhibitor with minimal cross-reactivity for the constitutive proteasome.

研究领域

产品类型

定制您的化合物库

Carfilzomib (PR-171)

客户使用Selleck生产的Carfilzomib (PR-171)发表文献140篇：

产品安全说明书

Proteasome抑制剂选择性比较

生物活性

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

参考文献

溶解度 (25°C)

化学数据 Download Carfilzomib (PR-171) SDF

动物体内配方计算器 (澄清溶液)

计算器

摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

稀释计算器

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

连续稀释计算器方程

连续稀释

计算结果

分子量计算器

总分子量：g/mol

摩尔浓度计算器

临床试验信息 (data from https://clinicaltrials.gov, updated on 2021-01-06)

技术支持

常见问题及建议解决方法

Proteasome Signaling Pathway Map

Proteasome Inhibitors with Unique Features

相关Proteasome产品