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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3 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.

    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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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 M4nGcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2K4d|AuOTByIH7N M4H1XFQ5KGh? MXzJR|UxyqB;wrCxNEBvVQ>? NIK3[nczPTNzMkW0Ny=>
NCI-H929  NU\leoFwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvjSYV2OC1zMECgcm0> M3nqWFQ5KGh? NGTpXldKSzVyIE5CpFE1KG6P MXqyOVMyOjV2Mx?=
SUDHL16  MXrBdI9xfG:|aYOgRZN{e2G7 MYGyMlXjiJN|LkWgcm0> M4eyfVQ5KGh? M4fIcoVvcGGwY3XzJJRp\SClZXzsJIRm[XSqIHPvMZRz\WG2bXXueEB4cXSqIFHDXVEzOTV? NGnkVnEzPTJ|OUmzOS=>
SUDHL14 MVLBdI9xfG:|aYOgRZN{e2G7 Mn[xNk426oDVMz61JI5O MUS0PEBp NXnRN|NV\W6qYX7j[ZMhfGinIHPlcIwh\GWjdHigZ48ufHKnYYTt[Y51KHerdHigRWN[OTJzNR?= NG\KUXQzPTJ|OUmzOS=>
U2932 NV\nbmJFSXCxcITvd4l{KEG|c4PhfS=> NX\kcXc{Oi534pETN{42KG6P M1zhc|Q5KGh? MXrlcohidmOnczD0bIUh[2WubDDk[YF1cCClbz30doVifG2nboSge4l1cCCDQ2mxNlE2 NGHYcowzPTJ|OUmzOS=>
P-UMSCC-1 NFrXO|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTFzLkKgcm0> MnTNNlQ6OTVyM{m=
R-UMSCC-1 NHuyUo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX7l[YQ{UUN3ME2yNlk1KG6P NVvseVVGOjR7MUWwN|k>
P-Cal33 Ml32S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH7Wd2JKSzVyPUG3MlMhdk1? NIP6coszPDlzNUCzPS=>
R-Cal33 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTFzMUKgcm0> NHqxeI0zPDlzNUCzPS=>
Jurkat M33CN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjEdFN2OS1zMX7N MoDMOFghcA>? NYr4PY1{cW6qaXLpeJMhfGinIHPlcIwheHKxbHnm[ZJifGmxbjDjc{11emWjdH3lcpQhf2m2aDD2c5Jqdm:|dHH0 M2nmXlI1QDBzMUK4
Jurkat NX7v[IRRSXCxcITvd4l{KEG|c4PhfS=> M3HXRVghdk1? MYmyOE81QCCq MWfpcoR2[2W|IHHwc5B1d3OrczygZ4F{eGG|ZTDhZ5RqfmG2aX;uMEBidmRiUFHSVEBkdGWjdnHn[UBkdy22cnXheI1mdnRid3n0bEB3d3Krbn;zeIF1 M2XjPFI1QDBzMUK4
UMSCC-22A NVfKTJhISXCxcITvd4l{KEG|c4PhfS=> MYOyNFAhdk1? MnXKNlQhcA>? NI\3cI9qdmS3Y3WgeIhmKGOnbHygZZBweHSxc3nzJINwNXS{ZXH0cYVvfCC5aYToJG9PYCByOUGy NES2XIwzOjl{OUiwNy=>
UMSCC-22B NULFXplVSXCxcITvd4l{KEG|c4PhfS=> MoLFNlAxKG6P NGL0XmozPCCq MnLobY5lfWOnIITo[UBk\WyuIHHwc5B1d3OrczDjc{11emWjdH3lcpQhf2m2aDDPUnghODlzMh?= NU[3XolqOjJ7Mkm4NFM>
1483 NUHGXo5HSXCxcITvd4l{KEG|c4PhfS=> MmnONlAxKG6P MWOyOEBp NWfLSWhjcW6mdXPlJJRp\SClZXzsJIFxd3C2b4Ppd{Bkdy22cnXheI1mdnRid3n0bEBQVlhiMEmxNi=> NYfTPWg4OjJ7Mkm4NFM>
UMSCC-1 NVH2OWlqSXCxcITvd4l{KEG|c4PhfS=> M1TnTFIxOCCwTR?= MYmyOEBp M1TESYlv\HWlZTD0bIUh[2WubDDhdI9xfG:|aYOgZ48ufHKnYYTt[Y51KHerdHigU25ZKDB7MUK= MmHINlI6Ojl6MEO=
UMSCC-22A MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHS0RpNKSzVyPUO4MlchyrFiMT6wJI5O NF\5WYQzOjl{OUiwNy=>
UMSCC-22B NYfjUXJ[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVXJR|UxRTNyLkegxtEhQS5|IH7N NGmxUGczOjl{OUiwNy=>
1483 MlvZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXrQ[ZFXUUN3ME21NE42KMLzIEGxMlkhdk1? MoD5NlI6Ojl6MEO=
UMSCC-1 Mn;ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUOxUJlvUUN3ME2zOE43KMLzIEKuOkBvVQ>? M2PMZ|IzQTJ7OECz
Cal33 NWKyblFLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWLSWXZQUUN3ME20PU4{KMLzIEiuPUBvVQ>? NF3UXXczOjl{OUiwNy=>
PCI-15A MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF63TnFKSzVyPUewMlQhyrFiMkKuOkBvVQ>? NI\RSoszOjl{OUiwNy=>
PCI-15B NV\nbJNzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX;NV|ZrUUN3ME2zPU42KMLzIEGxMlAhdk1? MV2yNlkzQThyMx?=
OSC-19 MkjYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXXtZ49IUUN3ME2xPE4{KMLzIESuNkBvVQ>? MUeyNlkzQThyMx?=
SUDHL16 MorsRZBweHSxc3nzJGF{e3OjeR?= M1\FWFIvOC12LkCgcm0> NIrD[mc1QCCq MmXHbY5lfWOnczDj[YxtKGSnYYToJINwNXS{ZXH0cYVvfCC5aYToJI9j[XSxY3zhfC=> MkmwNlI1OTF6OUm=
SUDHL16 MUjGeY5kfGmxbjDBd5NigQ>? NEHMdnozNjVibl2= M{HYZVI1KGh? MoTLZYN1cX[jdHXzJGpPUyxiaX7hZ5RqfmG2ZYOgRWtVNCC3cD3y[Yd2dGG2ZYOgUo95[SxiYX7kJIlv\HWlZYOg{tNJOkFwWDDjc{11emWjdH3lcpQhf2m2aDDvZoF1d2OuYYi= M{O2cVIzPDFzOEm5
Granta MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUPF[|UxOC12IH7N MlvwOFghcA>? NF\5c3NqdmS3Y3WgZ4VtdCCmZXH0bEBkdy22cnXheI1mdnRid3n0bEBJSUSFSYO= NUCzSnpuOjF5NUCyNlQ>
SUDHL16 M2jYfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYC3RZZxOS12IH7N NV7lVXI6OzZiaB?= NVLCbVg4cW6mdXPlJINmdGxiZHXheIgh[29vdILlZZRu\W62IIfpeIghUEGGQ1nz NE[2OlYzODJ|M{m3Ny=>

... 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 <1 mg/mL
Ethanol <1 mg/mL
In vivo 2% DMSO+castor oil 10mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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
NCT02802163 Not yet recruiting Multiple Myeloma H. Lee Moffitt Cancer Center and Research Institute|Novartis|Amgen April 30, 2017 Phase 1|Phase 2
NCT01402284 Active, not recruiting Multiple Myeloma National Cancer Institute (NCI)|Celgene|Onyx Therapeutics, Inc.|National Institutes of Health Clinical Center (CC) July 21, 2011 Phase 2
NCT03031730 Not yet recruiting Hypercalcemia|Plasmacytoma|Recurrent Plasma Cell Myeloma|Refractory Plasma Cell Myeloma National Cancer Institute (NCI) October 2017 Phase 1
NCT03029234 Not yet recruiting Relapsed and Refractory Multiple Myeloma Amgen|Onyx Therapeutics, Inc. February 2017 Phase 3
NCT02891811 Not yet recruiting Multiple Myeloma Arbeitsgemeinschaft medikamentoese Tumortherapie|Amgen January 2017 Phase 2
NCT03004287 Not yet recruiting Multiple Myeloma University of Arkansas|Janssen, LP January 2017 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID