Carfilzomib (PR-171) 化学構造
分子量: 719.91





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  • 研究分野



製品説明 Carfilzomib (PR-171) is a proteasome inhibitor with IC50 less than 5 nM.
ターゲット Proteasome
IC50 5 nM [1]
In vitro試験 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 LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
MM.1S MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3HBWlAuOTByIH7N NEm0XXM1QCCq NGjsfVhKSzVywrC9xsAyOCCwTR?= NYD3b3U4OjV|MUK1OFM>
SUDHL16  NGfrXoNCeG:ydH;zbZMhSXO|c3H5 MlrpNk426oDVMz61JI5O MnnTOFghcA>? NWnl[oo1\W6qYX7j[ZMhfGinIHPlcIwh\GWjdHigZ48ufHKnYYTt[Y51KHerdHigRWN[OTJzNR?= NH\Db2MzPTJ|OUmzOS=>
U2932 NEC3cYdCeG:ydH;zbZMhSXO|c3H5 MoHGNk426oDVMz61JI5O MUS0PEBp MVXlcohidmOnczD0bIUh[2WubDDk[YF1cCClbz30doVifG2nboSge4l1cCCDQ2mxNlE2 NWf5VnBzOjV{M{m5N|U>
P-UMSCC-1 NEnyUWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHfFSFNKSzVyPUGxMlIhdk1? NWfafWJbOjR7MUWwN|k>
R-UMSCC-1 M13kWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2XxTGlEPTB;MkK5OEBvVQ>? M4HvflI1QTF3MEO5
P-Cal33 NEDtW4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1r3TmlEPTB;MUeuN{BvVQ>? MWKyOFkyPTB|OR?=
R-Cal33 NX\jNZhGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoPTTWM2OD1zMUGyJI5O M1[0R|I1QTF3MEO5
Jurkat NX;DcGIyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoS0NU0yOW6P MnTBOFghcA>? MnntbY5pcWKrdIOgeIhmKGOnbHygdJJwdGmoZYLheIlwdiClbz30doVifG2nboSge4l1cCC4b4Lpco9{fGG2 NUfTd3EyOjR6MEGxNlg>
Jurkat MnnxRZBweHSxc3nzJGF{e3OjeR?= NET0T3c5KG6P MYGyOE81QCCq NUezfIoycW6mdXPld{BieG:ydH;zbZMtKGOjc4Dhd4Uh[WO2aY\heIlwdixiYX7kJHBCWlBiY3zlZZZi\2ViY3:teJJm[XSvZX70JJdqfGhidn;ybY5we3SjdB?= MkD0NlQ5ODFzMki=
UMSCC-22A MYfBdI9xfG:|aYOgRZN{e2G7 M{jHRVIxOCCwTR?= NWPnT29KOjRiaB?= MVzpcoR2[2VidHjlJINmdGxiYYDvdJRwe2m|IHPvMZRz\WG2bXXueEB4cXSqIF;OXEAxQTF{ MWiyNlkzQThyMx?=
1483 MXXBdI9xfG:|aYOgRZN{e2G7 NGWzc|czODBibl2= M3XTc|I1KGh? MVnpcoR2[2VidHjlJINmdGxiYYDvdJRwe2m|IHPvMZRz\WG2bXXueEB4cXSqIF;OXEAxQTF{ MkPaNlI6Ojl6MEO=
UMSCC-1 NUXMdmlvSXCxcITvd4l{KEG|c4PhfS=> NIrjVmgzODBibl2= NGjjXngzPCCq MUXpcoR2[2VidHjlJINmdGxiYYDvdJRwe2m|IHPvMZRz\WG2bXXueEB4cXSqIF;OXEAxQTF{ MXWyNlkzQThyMx?=
UMSCC-22A M4jwemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTN6LkegxtEhOS5yIH7N MnPkNlI6Ojl6MEO=
UMSCC-22B MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIPIXHJKSzVyPUOwMlchyrFiOT6zJI5O MnPiNlI6Ojl6MEO=
1483 M2nYU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmXlTWM2OD13MD61JOKyKDFzLkmgcm0> NV\0bHE5OjJ7Mkm4NFM>
UMSCC-1 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmXsTWM2OD1|ND62JOKyKDJwNjDuUS=> MV:yNlkzQThyMx?=
Cal33 MnnZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUnJR|UxRTR7LkOgxtEhQC57IH7N Mln2NlI6Ojl6MEO=
PCI-15B M2f4PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEHKTG5KSzVyPUO5MlUhyrFiMUGuNEBvVQ>? NGCxV4QzOjl{OUiwNy=>
OSC-19 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2nnZ2lEPTB;MUiuN{DDuSB2LkKgcm0> NWK0RZVyOjJ7Mkm4NFM>
SUDHL16 M1nMeWFxd3C2b4Ppd{BCe3O|YYm= MnHkNk4xNTRwMDDuUS=> M3XZblQ5KGh? Mm\nbY5lfWOnczDj[YxtKGSnYYToJINwNXS{ZXH0cYVvfCC5aYToJI9j[XSxY3zhfC=> MV:yNlQyOTh7OR?=
SUDHL16 MnXUSpVv[3Srb36gRZN{[Xl? NWD3S3dbOi53IH7N MX:yOEBp MVThZ5RqfmG2ZYOgTm5MNCCrbnHjeIl3[XSnczDBT3QtKHWyLYLl[5Vt[XSnczDOc5hiNCCjbnSgbY5lfWOnczFOt2gzSS6[IHPvMZRz\WG2bXXueEB4cXSqIH;iZZRw[2yjeB?= MmXiNlI1OTF6OUm=
Granta NVy0enk1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEO4NI4xNTRibl2= M2jKXlQ5KGh? M37nRolv\HWlZTDj[YxtKGSnYYToJINwNXS{ZXH0cYVvfCC5aYToJGhCTEOLcx?= M3P1blIyPzVyMkK0
SUDHL16 NGrTVZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1W1UlEuPCCwTR?= NWHpVHc6OzZiaB?= MUTpcoR2[2ViY3XscEBl\WG2aDDjc{11emWjdH3lcpQhf2m2aDDIRWREUXN? M1HrWlIxOjN|OUez

... Click to View More Cell Line Experimental Data

In vivo試験 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]
臨床試験 Carfilzomib has entered in a Phase II clinical trial in the treatment of multiple myeloma.

プロトコル (参考用のみ)

キナーゼアッセイ: [1]

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.

細胞アッセイ: [1]

細胞株 WST-1, ANBL-6 cells
濃度 100 nM
反応時間 1 hour
実験の流れ 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.

動物実験: [4]

動物モデル Beige-nude-XID mice
製剤 10% sulfobutylether β-cyclodextrin in 10 mmol/L citrate buffer pH 3.5,
投薬量 2.0 mg/kg
投与方法 i.v.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)



Download Carfilzomib (PR-171) SDF
分子量 719.91


CAS No. 868540-17-4
保管 3年-20℃
2年-80℃in solvent
別名 N/A
溶解度 (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.
化学名 L-Phenylalaninamide, (αS)-α-[[2-(4-morpholinyl)acetyl]amino]benzenebutanoyl-L-leucyl-N-[(1S)-3-methyl-1-[[(2R)-2-methyl-2-oxiranyl]carbonyl]butyl]-

文献中の引用 (18)

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.



電話番号: +1-832-582-8158 Ext:3月曜日〜金曜日 9:00 AM–5:00 PM (米国中部標準時)


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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID