Carfilzomib (PR-171)

製品コードS2853

Carfilzomib (PR-171)化学構造

分子量(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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JPY 79016.00
JPY 28220.00
JPY 44820.00
JPY 111220.00
JPY 144420.00

カスタマーフィードバック(5)

  • 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.

製品安全説明書

Proteasome阻害剤の選択性比較

生物活性

製品説明 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.
ターゲット
Proteasome [1]
(ANBL-6 cells)
5 nM
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MM.1S MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHHufHAxNTFyMDDuUS=> MUO0PEBp NEi0R2pKSzVywrC9xsAyOCCwTR?= NFfPNlgzPTNzMkW0Ny=>
NCI-H929  NFTTenlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHrFSmQxNTFyMDDuUS=> MXW0PEBp MYfJR|UxKD4EoEG0JI5O MkHQNlU{OTJ3NEO=
SUDHL16  NELZOJhCeG:ydH;zbZMhSXO|c3H5 Ml\RNk426oDVMz61JI5O Mk\2OFghcA>? M{PPZoVvcGGwY3XzJJRp\SClZXzsJIRm[XSqIHPvMZRz\WG2bXXueEB4cXSqIFHDXVEzOTV? NG\IWmszPTJ|OUmzOS=>
SUDHL14 NGi3UIhCeG:ydH;zbZMhSXO|c3H5 M1fr[|IvPeLCk{OuOUBvVQ>? M1nDVFQ5KGh? NHnYVopmdmijbnPld{B1cGViY3XscEBl\WG2aDDjc{11emWjdH3lcpQhf2m2aDDBR3kyOjF3 MmfsNlUzOzl7M{W=
U2932 M2jjOGFxd3C2b4Ppd{BCe3O|YYm= MkC5Nk426oDVMz61JI5O NH;6UJk1QCCq NGPDcHJmdmijbnPld{B1cGViY3XscEBl\WG2aDDjc{11emWjdH3lcpQhf2m2aDDBR3kyOjF3 MWmyOVI{QTl|NR?=
P-UMSCC-1 NXuzVWV7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnJR|UxRTFzLkKgcm0> NXPMdXVTOjR7MUWwN|k>
R-UMSCC-1 NU\xOGFCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoXmTWM2OD1{Mkm0JI5O NUGxWJJFOjR7MUWwN|k>
P-Cal33 NHXRUo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXvEeYU6UUN3ME2xO{4{KG6P NXq3[JpDOjR7MUWwN|k>
R-Cal33 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlXtTWM2OD1zMUGyJI5O NHHNeGEzPDlzNUCzPS=>
Jurkat M2DBcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\G[WkyNTFzbl2= M{O4XlQ5KGh? MYXpcohq[mm2czD0bIUh[2WubDDwdo9tcW[ncnH0bY9vKGOxLYTy[YF1dWWwdDD3bZRpKH[xcnnuc5N1[XR? MXGyOFgxOTF{OB?=
Jurkat MmnxRZBweHSxc3nzJGF{e3OjeR?= M4DONVghdk1? MlmwNlQwPDhiaB?= MXXpcoR2[2W|IHHwc5B1d3OrczygZ4F{eGG|ZTDhZ5RqfmG2aX;uMEBidmRiUFHSVEBkdGWjdnHn[UBkdy22cnXheI1mdnRid3n0bEB3d3Krbn;zeIF1 MXKyOFgxOTF{OB?=
UMSCC-22A NIDJT5dCeG:ydH;zbZMhSXO|c3H5 NGnlfG4zODBibl2= MnThNlQhcA>? NVnZRllPcW6mdXPlJJRp\SClZXzsJIFxd3C2b4Ppd{Bkdy22cnXheI1mdnRid3n0bEBQVlhiMEmxNi=> M13sWlIzQTJ7OECz
UMSCC-22B MkGxRZBweHSxc3nzJGF{e3OjeR?= MWSyNFAhdk1? M3\kRlI1KGh? NHH1N|RqdmS3Y3WgeIhmKGOnbHygZZBweHSxc3nzJINwNXS{ZXH0cYVvfCC5aYToJG9PYCByOUGy M{Pzd|IzQTJ7OECz
1483 NF;USJlCeG:ydH;zbZMhSXO|c3H5 MVyyNFAhdk1? NFzIRowzPCCq NX;vb5k1cW6mdXPlJJRp\SClZXzsJIFxd3C2b4Ppd{Bkdy22cnXheI1mdnRid3n0bEBQVlhiMEmxNi=> Mnm4NlI6Ojl6MEO=
UMSCC-1 NVr6O3I5SXCxcITvd4l{KEG|c4PhfS=> MUeyNFAhdk1? NULEbGhsOjRiaB?= MVHpcoR2[2VidHjlJINmdGxiYYDvdJRwe2m|IHPvMZRz\WG2bXXueEB4cXSqIF;OXEAxQTF{ MViyNlkzQThyMx?=
UMSCC-22A M{n3UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV[0SWFwUUN3ME2zPE44KMLzIEGuNEBvVQ>? Mnf5NlI6Ojl6MEO=
UMSCC-22B NY\CfotuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1nyfGlEPTB;M{CuO{DDuSB7LkOgcm0> NWroSVBROjJ7Mkm4NFM>
1483 M2LiTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MorhTWM2OD13MD61JOKyKDFzLkmgcm0> NUTwdGhDOjJ7Mkm4NFM>
UMSCC-1 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUjJR|UxRTN2Lk[gxtEhOi54IH7N MUGyNlkzQThyMx?=
Cal33 NGj1dmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1z1e2lEPTB;NEmuN{DDuSB6Lkmgcm0> MlzhNlI6Ojl6MEO=
PCI-15A Mo[xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3Lm[WlEPTB;N{CuOEDDuSB{Mj62JI5O M1jJO|IzQTJ7OECz
PCI-15B M{\wZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{fJXmlEPTB;M{muOUDDuSBzMT6wJI5O MmHINlI6Ojl6MEO=
OSC-19 M4rkbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4jlZWlEPTB;MUiuN{DDuSB2LkKgcm0> NFzy[W8zOjl{OUiwNy=>
SUDHL16 NF7C[mdCeG:ydH;zbZMhSXO|c3H5 NEX5XXQzNjBvND6wJI5O NUDsOJdWPDhiaB?= Mm\6bY5lfWOnczDj[YxtKGSnYYToJINwNXS{ZXH0cYVvfCC5aYToJI9j[XSxY3zhfC=> M2HBZVIzPDFzOEm5
SUDHL16 MVzGeY5kfGmxbjDBd5NigQ>? M3y0NFIvPSCwTR?= MkLhNlQhcA>? NYDrUG5u[WO2aY\heIV{KEqQSzygbY5i[3SrdnH0[ZMhSUuWLDD1dE1z\We3bHH0[ZMhVm:6YTygZY5lKGmwZIXj[ZMh|rOKMlGuXEBkdy22cnXheI1mdnRid3n0bEBw[mG2b3PsZZg> MXqyNlQyOTh7OR?=
Granta NYDiV21kT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2L4R|AuPCCwTR?= M2rWclQ5KGh? NIjlZodqdmS3Y3WgZ4VtdCCmZXH0bEBkdy22cnXheI1mdnRid3n0bEBJSUSFSYO= MnOyNlE4PTB{MkS=
SUDHL16 M2DER2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3e4UFEuPCCwTR?= NXT4fo9DOzZiaB?= MkfEbY5lfWOnIHPlcIwh\GWjdHigZ48ufHKnYYTt[Y51KHerdHigTGFFS0m| M4fwO|IxOjN|OUez

他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

体内試験 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]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[1]
+ 展開

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.
細胞試験: [1]
+ 展開
  • 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.
    (参考用のみ)
動物試験:[4]
+ 展開
  • 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.
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 50 mg/mL (69.45 mM)
Water Insoluble
Ethanol Insoluble
体内 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
2% DMSO+30% PEG 300+2%Tween 80+ddH2O
混合させたのち直ちに使用することを推奨します。
1mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 719.91
化学式

C40H57N5O7

CAS No. 868540-17-4
保管
in solvent
別名 N/A

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (g) = 濃度 (mol/L) x 体積 (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • 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):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

臨床試験

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

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

よくある質問(FAQ)

  • 質問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.

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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID