Carfilzomib (PR-171)

Catalog No.S2853

Carfilzomib (PR-171) Chemical Structure

Molecular Weight(MW): 719.91

Carfilzomib (PR-171) is an irreversible proteasome inhibitor with IC50 of <5 nM in ANBL-6 cells, 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.

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In DMSO USD 476 In stock
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5 Customer Reviews

  • Validation of activity and specificity of chemical inhibitors of; ATM, ATR, and DNAPK. H460 cells were treated with 1 uM camptothecin (CPT) or 20 ug/ml bleomycin for 1 h in the presence of the indicated inhibitors: DNAPK-i1—NU7026, DNAPK-i2—NU7441. MSH6,

    Sci Transl Med 2014 6(250), 250ra112. Carfilzomib (PR-171) purchased from Selleck.

    Immunoblot analysis of EZH2 in MM.1S cells treated with the indicated doses of carfilzomib for 24 hours. GAPDH served as a loading control.

    Clin Cancer Res, 2017, 23(16):4817-4830. Carfilzomib (PR-171) purchased from Selleck.

  • Immunoblot analysis of EZH2 in MM.1S cells treated with the indicated doses of carfilzomib for 24 hours. GAPDH served as a loading control.

    Clin Cancer Res, 2017, 23(16):4817-4830. Carfilzomib (PR-171) purchased from Selleck.

    MM.1S cells were treated with or without carfilzomib (10 nM) in the presence or absence of TAS-117 (0.5 uM) for 24 h. Whole cell lysates were subjected to western blotting using CHOP, PARP, and GAPDH Abs.The graph represents fold changes of CHOP density relative to GAPDH.

    Cancer Res 2014 74(16), 4458-69. Carfilzomib (PR-171) purchased from Selleck.

  • Transduction at 24 h is indicated as normalized luciferase activity. HeLa cells were cotreated with 1 uM Carfilzomib and 500 vg/cell rAAV2-EGFP, and transduction was analyzed by flow cytometry at 24 h. Bright-field and EGPF fluorescence images at 24 h postransduction of cells visually indicating transduction.

    J Virol 2013 87(23), 13035-41. Carfilzomib (PR-171) purchased from Selleck.

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Choose Selective Proteasome Inhibitors

Biological Activity

Description Carfilzomib (PR-171) is an irreversible proteasome inhibitor with IC50 of <5 nM in ANBL-6 cells, 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.
Targets
Proteasome [1]
(ANBL-6 cells)
5 nM
In vitro

Carfilzomib inhibits proliferation in a variety of cell lines and patient-derived neoplastic cells, including multiple myeloma, and induced intrinsic and extrinsic apoptotic signaling pathways and activation of c-Jun-N-terminal kinase (JNK). Carfilzomib reveals enhanced anti-MM activity compared with bortezomib, overcome resistance to bortezomib and other agents, and acts synergistically with dexamethasone (Dex). Carfilzomib shoes preferential in vitro inhibitory potency against the ChT-L activity in the β5 subunit, with over 80% inhibition at doses of 10 nM. Short exposure to low-dose Carfilzomib leads to preferential binding specificity for the β5 constitutive 20S proteasome and the β5i immunoproteasome subunits. Measurement of caspase activity in ANBL-6 cells pulsed with Carfilzomib reveals substantial increases in caspase-8, caspase-9, and caspase-3 activity after 8 hours, giving a 3.2-, 3.9- and 6.9-fold increase, respectively, over control cells after 8 hours. In carfilzomib pulse-treated cells, the mitochondrial membrane integrity is decreased to 41% (Q1 + Q2), compared with 75% in vehicle-treated control cells. [1] In another study, Carfilzomib has also shown preclinical effectiveness against hematological and solid malignancies. [2] Carfilzomib directly inhibits osteoclasts formation and bone resorption. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MM.1S NWDiUI84T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\FdVAuOTByIH7N MWS0PEBp Mm\STWM2OMLiPdMgNVAhdk1? MVWyOVMyOjV2Mx?=
NCI-H929  MoHVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3W1flAuOTByIH7N MkfBOFghcA>? MkPKTWM2OCB;wrCxOEBvVQ>? NX3OemNVOjV|MUK1OFM>
SUDHL16  NECybnNCeG:ydH;zbZMhSXO|c3H5 M{P4ZlIvPeLCk{OuOUBvVQ>? MoLVOFghcA>? NEL3[WhmdmijbnPld{B1cGViY3XscEBl\WG2aDDjc{11emWjdH3lcpQhf2m2aDDBR3kyOjF3 NV[5[446OjV{M{m5N|U>
SUDHL14 MnXyRZBweHSxc3nzJGF{e3OjeR?= NELQXGEzNjYkgKOzMlUhdk1? Mo\ROFghcA>? NE[ySG5mdmijbnPld{B1cGViY3XscEBl\WG2aDDjc{11emWjdH3lcpQhf2m2aDDBR3kyOjF3 M4nt[lI2OjN7OUO1
U2932 NWrwbo9TSXCxcITvd4l{KEG|c4PhfS=> M3rQc|IvPeLCk{OuOUBvVQ>? NW\HN2RpPDhiaB?= NETXVHBmdmijbnPld{B1cGViY3XscEBl\WG2aDDjc{11emWjdH3lcpQhf2m2aDDBR3kyOjF3 M4nrN|I2OjN7OUO1
P-UMSCC-1 MkLhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTpTWM2OD1zMT6yJI5O M4jMe|I1QTF3MEO5
R-UMSCC-1 NHXZVFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2LzUGlEPTB;MkK5OEBvVQ>? MoHHNlQ6OTVyM{m=
P-Cal33 M3rubWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGL2cZRKSzVyPUG3MlMhdk1? NIHzPJozPDlzNUCzPS=>
R-Cal33 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTFzMUKgcm0> MXeyOFkyPTB|OR?=
Jurkat M3Pk[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVOxMVEydk1? NYjOVFVSPDhiaB?= MoHYbY5pcWKrdIOgeIhmKGOnbHygdJJwdGmoZYLheIlwdiClbz30doVifG2nboSge4l1cCC4b4Lpco9{fGG2 MoW4NlQ5ODFzMki=
Jurkat M13BNGFxd3C2b4Ppd{BCe3O|YYm= MX[4JI5O M4[3T|I1NzR6IHi= MmSybY5lfWOnczDhdI9xfG:|aYOsJINie3Cjc3WgZYN1cX[jdHnvckwh[W6mIGDBVnAh[2ynYY\h[4Uh[29vdILlZZRu\W62IIfpeIghfm:{aX7vd5RifA>? NYO4UWFJOjR6MEGxNlg>
UMSCC-22A NUL4No1qSXCxcITvd4l{KEG|c4PhfS=> NFzBSFIzODBibl2= MlGzNlQhcA>? NInuS|JqdmS3Y3WgeIhmKGOnbHygZZBweHSxc3nzJINwNXS{ZXH0cYVvfCC5aYToJG9PYCByOUGy MXOyNlkzQThyMx?=
UMSCC-22B NHzXPG9CeG:ydH;zbZMhSXO|c3H5 MnTINlAxKG6P NFzBNpEzPCCq MXfpcoR2[2VidHjlJINmdGxiYYDvdJRwe2m|IHPvMZRz\WG2bXXueEB4cXSqIF;OXEAxQTF{ NYTYOHJMOjJ7Mkm4NFM>
1483 MoHLRZBweHSxc3nzJGF{e3OjeR?= MXiyNFAhdk1? NXmyUo1yOjRiaB?= NXfVdJNGcW6mdXPlJJRp\SClZXzsJIFxd3C2b4Ppd{Bkdy22cnXheI1mdnRid3n0bEBQVlhiMEmxNi=> MVuyNlkzQThyMx?=
UMSCC-1 NUH1UFRxSXCxcITvd4l{KEG|c4PhfS=> NELYTFMzODBibl2= M{Ls[VI1KGh? NUHEfYFxcW6mdXPlJJRp\SClZXzsJIFxd3C2b4Ppd{Bkdy22cnXheI1mdnRid3n0bEBQVlhiMEmxNi=> M1THbFIzQTJ7OECz
UMSCC-22A MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXnOd5diUUN3ME2zPE44KMLzIEGuNEBvVQ>? NYT1UZA1OjJ7Mkm4NFM>
UMSCC-22B NEDwR4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWHJR|UxRTNyLkegxtEhQS5|IH7N M3HiVFIzQTJ7OECz
1483 NV;ldoJMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M37BemlEPTB;NUCuOUDDuSBzMT65JI5O MWKyNlkzQThyMx?=
UMSCC-1 NWPSOJVRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmrBTWM2OD1|ND62JOKyKDJwNjDuUS=> M1L6XVIzQTJ7OECz
Cal33 M12zb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXTw[oEzUUN3ME20PU4{KMLzIEiuPUBvVQ>? MUmyNlkzQThyMx?=
PCI-15A Mk\6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmPOTWM2OD15MD60JOKyKDJ{Lk[gcm0> NWjtemNVOjJ7Mkm4NFM>
PCI-15B M{L6RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlr0TWM2OD1|OT61JOKyKDFzLkCgcm0> M2\0UlIzQTJ7OECz
OSC-19 NXTiSJNMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUnyOJlLUUN3ME2xPE4{KMLzIESuNkBvVQ>? NYXFVZExOjJ7Mkm4NFM>
SUDHL16 MkTKRZBweHSxc3nzJGF{e3OjeR?= NGjETokzNjBvND6wJI5O MmOyOFghcA>? NXnyfmoxcW6mdXPld{Bk\WyuIHTlZZRpKGOxLYTy[YF1dWWwdDD3bZRpKG:kYYTvZ4xigA>? M4XFO|IzPDFzOEm5
SUDHL16 NITWcm9HfW6ldHnvckBCe3OjeR?= NX;SOnhOOi53IH7N MlPuNlQhcA>? NYHEd445[WO2aY\heIV{KEqQSzygbY5i[3SrdnH0[ZMhSUuWLDD1dE1z\We3bHH0[ZMhVm:6YTygZY5lKGmwZIXj[ZMh|rOKMlGuXEBkdy22cnXheI1mdnRid3n0bEBw[mG2b3PsZZg> MVeyNlQyOTh7OR?=
Granta M4PHOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljlNE01KG6P Mo[2OFghcA>? M4O2Uolv\HWlZTDj[YxtKGSnYYToJINwNXS{ZXH0cYVvfCC5aYToJGhCTEOLcx?= MY[yNVc2ODJ{NB?=
SUDHL16 NVjyTY5tT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWSxMVQhdk1? MmHTN|YhcA>? MXPpcoR2[2ViY3XscEBl\WG2aDDjc{11emWjdH3lcpQhf2m2aDDIRWREUXN? MkHXNlAzOzN7N{O=

... Click to View More Cell Line Experimental Data

In vivo Carfilzomib moderately reduces tumor growth in an in vivo xenograft model. Carfilzomib effectively decreases multiple myeloma cell viability following continual or transient treatment mimicking. Carfilzomib increases trabecular bone volume, decreases bone resorption and enhances bone formation in non-tumor bearing mice. [3]

Protocol

Kinase Assay:[1]
+ Expand

Enzyme-linked immunosorbent assay for subunit profiling of carfilzomib:

ANBL-6 cells (2 × 106/well) are plated in 96-well plates and treated with Carfilzomib doses from 0.001 to 10 μM for 1 hour. Cells are then lysed (20 mM Tris-HCl, 0.5 mM EDTA), and cleared lysates are transferred to polymerase chain reaction (PCR) plates. A standard curve is generated using untreated ANBL-6 cell lysates starting at a concentration of 6 μg protein/μL. The active site probe [biotin-(CH2)4-Leu-Leu-Leu-epoxyketone; 20 μM] is added and incubated at room temperature for 1 hour. Cell lysates are then denatured by adding 1% sodium dodecyl sulfate (SDS) and heating to 100°C, followed by mixing with 20 μL per well streptavidin-sepharose high-performance beads in a 96-well multiscreen DV plate and incubated for 1 hour. These beads are then washed with enzyme-linked immunosorbent assay (ELISA) buffer (PBS, 1% bovine serum albumin, and 0.1% Tween-20), and incubated overnight at 4°C on a plate shaker with antibodies to proteasome subunits. Antibodies used included mouse monoclonal anti-β1, anti-β2, anti-β1i, and anti-β5i, goat polyclonal anti-β2i, and rabbit polyclonal anti-β5 (affinity-purified antiserum against KLH-CWIRVSSDNVADLHDKYS peptide). The beads are washed and incubated for 2 hours with horseradish peroxidase-conjugated secondary goat antirabbit, goat antimouse or rabbit antigoat antibodies. After washing, the beads are developed using the supersignal ELISA picochemiluminescence substrate. Luminescent detection is performed. Raw luminescence is converted to μg/mL by comparison with the standard curve and expressed as the % inhibition relative to vehicle control. Curve fits are generated using the following nonsigmoidal dose-response equation: Y = Bottom + (Top-Bottom)/(1 + 10̂((LogEC50 − X) × HillSlope)), where X is the logarithm of concentration, Y is the % inhibition, and EC50 is the dose showing 50% effect.
Cell Research:[1]
+ Expand
  • Cell lines: WST-1, ANBL-6 cells
  • Concentrations: 100 nM
  • Incubation Time: 1 hour
  • Method: WST-1 is used to determine the effects of proteasome inhibitor Carfilzomib on cell proliferation. The inhibition of proliferation is calculated in relation to parallel control cells that receives vehicle alone. A linear spline function is used to interpolate the median inhibitory concentration (IC50) using XLfit 4 software. The degree of resistance (DOR) is calculated using the formula: DOR = IC50(resistant cells)/IC50(sensitive cells). ANBL-6 cells pulsed with 100 nM carfilzomib are washed and suspended in PBS containing 5 μg/mL of JC-1, which exhibits potential-dependent accumulation in mitochondria. Analysis of the mitochondrial membrane potential-dependent color shift from 525 to 590 nm is carried out on a FacScan, and the data are analyzed with CellQuest software.
    (Only for Reference)
Animal Research:[4]
+ Expand
  • Animal Models: Beige-nude-XID mice
  • Formulation: 10% sulfobutylether β-cyclodextrin in 10 mmol/L citrate buffer pH 3.5,
  • Dosages: 2.0 mg/kg
  • Administration: i.v.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 50 mg/mL (69.45 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+2%Tween 80+ddH2O
For best results, use promptly after mixing.
1mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 719.91
Formula

C40H57N5O7

CAS No. 868540-17-4
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03729804 Not yet recruiting Multiple Myeloma University of Chicago December 24 2018 Phase 3
NCT03673826 Not yet recruiting Smouldering Myeloma Stichting Hemato-Oncologie voor Volwassenen Nederland November 2018 Phase 2
NCT03606577 Not yet recruiting Multiple Myeloma Nantes University Hospital November 2 2018 Phase 2
NCT03605719 Recruiting Recurrent Plasma Cell Myeloma Emory University|Bristol-Myers Squibb|Oncolytics Biotech|University of Utah|City of Hope Medical Center|Phylogeny October 24 2018 Phase 1
NCT03500445 Not yet recruiting Myeloma|Multiple Myeloma University of Chicago October 2018 Phase 2
NCT03742297 Recruiting Newly Diagnosed Multiple Myeloma PETHEMA Foundation October 22 2018 Phase 3

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Frequently Asked Questions

  • Question 1:

    How should I prepare solution of Carfilzomib for ongoing in vivo study?

  • Answer:

    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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID