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)は一種の不可逆的なプロテアソーム( proteasome)阻害剤で、ANBL-6細胞にIC50値が5nM以下ですが、体外でβ5ユニットのChT-L活性を優先に抑制して、PGPHとT-Lに作用する活性が弱い或いはないです。

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JPY 68538.28 あり
JPY 24477.96 あり
JPY 38876.76 あり
JPY 96471.96 あり
JPY 125269.56 あり

カスタマーフィードバック(3)

  • 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.

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)は一種の不可逆的なプロテアソーム( proteasome)阻害剤で、ANBL-6細胞にIC50値が5nM以下ですが、体外でβ5ユニットのChT-L活性を優先に抑制して、PGPHとT-Lに作用する活性が弱い或いはないです。
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 NVnuS4U5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{DONFAuOTByIH7N NV3BTY9bPDhiaB?= NYfOOYx3UUN3MNMgQeKhOTBibl2= MoDUNlU{OTJ3NEO=
NCI-H929  NVTKeFJFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\XOlAuOTByIH7N NUnIdGlCPDhiaB?= MVvJR|UxKD4EoEG0JI5O NGXhNnQzPTNzMkW0Ny=>
SUDHL16  M4X5eGFxd3C2b4Ppd{BCe3O|YYm= NGrMcogzNjYkgKOzMlUhdk1? MlPDOFghcA>? M12xXIVvcGGwY3XzJJRp\SClZXzsJIRm[XSqIHPvMZRz\WG2bXXueEB4cXSqIFHDXVEzOTV? MUGyOVI{QTl|NR?=
SUDHL14 MofCRZBweHSxc3nzJGF{e3OjeR?= MUOyMlXjiJN|LkWgcm0> NGDKXo81QCCq Mk\E[Y5p[W6lZYOgeIhmKGOnbHyg[IVifGhiY3:teJJm[XSvZX70JJdqfGhiQVPZNVIyPQ>? NHizOW0zPTJ|OUmzOS=>
U2932 MYLBdI9xfG:|aYOgRZN{e2G7 NXX3S251Oi534pETN{42KG6P NEnXXZE1QCCq M2XxXIVvcGGwY3XzJJRp\SClZXzsJIRm[XSqIHPvMZRz\WG2bXXueEB4cXSqIFHDXVEzOTV? NUm3O5FKOjV{M{m5N|U>
P-UMSCC-1 NVjHc21CT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2XvZmlEPTB;MUGuNkBvVQ>? MVSyOFkyPTB|OR?=
R-UMSCC-1 M1;YRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MluxTWM2OD1{Mkm0JI5O M1jSXVI1QTF3MEO5
P-Cal33 NWn1WWRYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFT0UWZKSzVyPUG3MlMhdk1? M4jwUFI1QTF3MEO5
R-Cal33 M2n3dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTFzMUKgcm0> M1vmUVI1QTF3MEO5
Jurkat MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUjwVmVlOS1zMX7N MWC0PEBp M{PoUYlvcGmkaYTzJJRp\SClZXzsJJBzd2yrZnXyZZRqd25iY3:teJJm[XSvZX70JJdqfGhidn;ybY5we3SjdB?= MkXSNlQ5ODFzMki=
Jurkat Ml3IRZBweHSxc3nzJGF{e3OjeR?= MnnLPEBvVQ>? NUL5TGpkOjRxNEigbC=> NIfKOHFqdmS3Y3XzJIFxd3C2b4Ppd{wh[2G|cHHz[UBi[3SrdnH0bY9vNCCjbnSgVGFTWCClbHXheoFo\SClbz30doVifG2nboSge4l1cCC4b4Lpco9{fGG2 NVLFcJVOOjR6MEGxNlg>
UMSCC-22A NVnpTVJ[SXCxcITvd4l{KEG|c4PhfS=> NV;sRYQ2OjByIH7N MkLXNlQhcA>? NH\LOWVqdmS3Y3WgeIhmKGOnbHygZZBweHSxc3nzJINwNXS{ZXH0cYVvfCC5aYToJG9PYCByOUGy NWTnOYFQOjJ7Mkm4NFM>
UMSCC-22B NFSySVZCeG:ydH;zbZMhSXO|c3H5 NFHmcowzODBibl2= NV7aXFB6OjRiaB?= NV\rNXJjcW6mdXPlJJRp\SClZXzsJIFxd3C2b4Ppd{Bkdy22cnXheI1mdnRid3n0bEBQVlhiMEmxNi=> MWiyNlkzQThyMx?=
1483 MWfBdI9xfG:|aYOgRZN{e2G7 NXnSNlE{OjByIH7N NHS5WnEzPCCq M3naS4lv\HWlZTD0bIUh[2WubDDhdI9xfG:|aYOgZ48ufHKnYYTt[Y51KHerdHigU25ZKDB7MUK= MUSyNlkzQThyMx?=
UMSCC-1 NInkTGVCeG:ydH;zbZMhSXO|c3H5 NEG0[nMzODBibl2= NIP2UHAzPCCq NHn0T5FqdmS3Y3WgeIhmKGOnbHygZZBweHSxc3nzJINwNXS{ZXH0cYVvfCC5aYToJG9PYCByOUGy NHHHco8zOjl{OUiwNy=>
UMSCC-22A NHvmbo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2XZVmlEPTB;M{iuO{DDuSBzLkCgcm0> M3vMS|IzQTJ7OECz
UMSCC-22B MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFr4S5ZKSzVyPUOwMlchyrFiOT6zJI5O M2r6PVIzQTJ7OECz
1483 NXTxelBjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4K2XmlEPTB;NUCuOUDDuSBzMT65JI5O MlHvNlI6Ojl6MEO=
UMSCC-1 MkDTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3nJV2lEPTB;M{SuOkDDuSB{Lk[gcm0> MVyyNlkzQThyMx?=
Cal33 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHmTWM2OD12OT6zJOKyKDhwOTDuUS=> Mn3BNlI6Ojl6MEO=
PCI-15A NWjUfmRFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUjJR|UxRTdyLkSgxtEhOjJwNjDuUS=> NHznT|IzOjl{OUiwNy=>
PCI-15B Ml3NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3zx[mlEPTB;M{muOUDDuSBzMT6wJI5O M{e0ZVIzQTJ7OECz
OSC-19 M4i3bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{O0bGlEPTB;MUiuN{DDuSB2LkKgcm0> NFjjO3QzOjl{OUiwNy=>
SUDHL16 MmjHRZBweHSxc3nzJGF{e3OjeR?= MknQNk4xNTRwMDDuUS=> MVK0PEBp MnKybY5lfWOnczDj[YxtKGSnYYToJINwNXS{ZXH0cYVvfCC5aYToJI9j[XSxY3zhfC=> MmfRNlI1OTF6OUm=
SUDHL16 M4nERWZ2dmO2aX;uJGF{e2G7 MoHwNk42KG6P M3zN[|I1KGh? Mm\VZYN1cX[jdHXzJGpPUyxiaX7hZ5RqfmG2ZYOgRWtVNCC3cD3y[Yd2dGG2ZYOgUo95[SxiYX7kJIlv\HWlZYOg{tNJOkFwWDDjc{11emWjdH3lcpQhf2m2aDDvZoF1d2OuYYi= MlfkNlI1OTF6OUm=
Granta NXq0V|FUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHXVb4kxNTRibl2= NWTscWhpPDhiaB?= MVrpcoR2[2ViY3XscEBl\WG2aDDjc{11emWjdH3lcpQhf2m2aDDIRWREUXN? NF7IVFMzOTd3MEKyOC=>
SUDHL16 M363Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\SOYQyNTRibl2= MXezOkBp NF;1NJdqdmS3Y3WgZ4VtdCCmZXH0bEBkdy22cnXheI1mdnRid3n0bEBJSUSFSYO= MkezNlAzOzN7N{O=

多くの細胞株試験データを見る場合、クリックしてください

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 順序で溶剤を入れること:
2% DMSO+castor oil
10mg/mL

* 溶解度検測はSelleck技術部門によって行いますので、文献より提供された溶解度と差異がある可能性がありますが、生産工芸と不同ロット(lot)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

解決のために必要とされるマス、ボリュームまたは濃度を計算してください。

マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • マス
    濃度
    ボリューム
    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

貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、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 ( 輸入 輸出 )

  • 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

マス 濃度 ボリューム 分子量

臨床試験

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

技術サポート

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

Handling Instructions

他の質問がある場合は、お気軽くお問合せください。

  • * 必須

よくある質問(FAQ)

  • 問題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信号経路図

Proteasome Inhibitors with Unique Features

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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