製品コードS1175 別名:CNF2024



BIIB021 is an orally available, fully synthetic small-molecule inhibitor of HSP90 with Ki and EC50 of 1.7 nM and 38 nM, respectively. Phase 2.

サイズ 価格(税別)  
JPY 19920.00
JPY 34860.00
JPY 69720.00
JPY 127820.00


  • PLoS Pathog 2012 8(11), e1003048. BIIB021 purchased from Selleck.

    PLoS Pathog 2012 8(11), e1003048. BIIB021 purchased from Selleck.

  • (G-I) WST-1 assays of MCF7 (G) with oPRL or 800 nM BIIB021 alone, (H) with DOX ± PRL, or (I) with DOX + BIIB021 ± PRL. n = 18. Data were analyzed with a one-way ANOVA followed by Bonferroni posttests. *P < 0.05; **P < 0.01; ***P < 0.001.

    Endocrinology, 2018, 159(2):907-930. BIIB021 purchased from Selleck.

    Acta Pharmacol Sin 2013 34(12), 1545-53. BIIB021 purchased from Selleck.

  • Acta Pharmacol Sin 2013 34(12), 1545-53. BIIB021 purchased from Selleck.

    Acta Pharmacol Sin 2013 34(12), 1545-53. BIIB021 purchased from Selleck.

  • Acta Pharmacol Sin 2013 34(12), 1545-53. BIIB021 purchased from Selleck.

    Molt-4 cells were cultured with or without varying concentrations of BIIB021 in 96-well plates for 24, 48, and 72 h, respectively. The antiproliferative effects were measured by the MTT assay. BIIB021 effectively inhibited Molt-4 cell growth in a dose- and time-dependent manner.

    Acta Pharmacol Sin 2013 34, 1545-53. BIIB021 purchased from Selleck.

  • The cells were treated with BIIB021 at 100 nmol/L and 200 nmol/L for 24 h and stained with PI. The DNA content was analyzed by flow cytometry.

    Acta Pharmacol Sin 2013 34, 1545-53. BIIB021 purchased from Selleck.

    Molt-4 cells were treated with BIIB021 at the indicated doses for 24 h, and apoptosis was assessed by flow cytometry using Annexin V/PI staining.The results showed that externalized PS, a characteristic of early apoptosis, was increased in the BIIB021-treated Molt-4 cells in a dose-dependent fashion.

    Acta Pharmacol Sin 2013 34, 1545-53. BIIB021 purchased from Selleck.


HSP (e.g. HSP90)阻害剤の選択性比較


製品説明 BIIB021 is an orally available, fully synthetic small-molecule inhibitor of HSP90 with Ki and EC50 of 1.7 nM and 38 nM, respectively. Phase 2.
HSP90 [1]
(Cell-free assay)
1.7 nM(Ki)

BIIB021 binds in the ATP-binding pocket of Hsp90, interferes with Hsp90 chaperone function, and results in client protein degradation and tumor growth inhibition. BIIB021 inhibits tumor cell (BT474, MCF-7, N87, HT29, H1650, H1299, H69 and H82) proliferation with IC50 from 0.06-0.31 μM. BIIB021 induces the degradation of Hsp90 client proteins including HER-2, Akt, and Raf-1 and up-regulated expression of the heat shock proteins Hsp70 and Hsp27. [1] BIIB021 inhibits Hodgkin's lymphoma cells (KM-H2, L428, L540, L540cy, L591, L1236 and DEV) with IC50 from 0.24-0.8 μM. BIIB021 shows low activity in lymphocytes from healthy individuals. BIIB021 inhibits the constitutive activity of NF-κB despite defective IκB. BIIB021 induces the expression of ligands for the activating NK cell receptor NKG2D on Hodgkin's lymphoma cells resulting in an increased susceptibility to NK cell–mediated killing. [2] BIIB021 enhanced the in vitro radiosensitivity of HNSCCA cell lines (UM11B and JHU12) with a corresponding reduction in the expression of key radioresponsive proteins, increased apoptotic cells and enhance G2 arrest. [3] BIIB021 is considerably more active than 17-AAG against adrenocortical carcinoma H295R, both in vitro and in vivo. The cytotoxic activity of BIIB021 is not influenced by loss of NQO1 or Bcl-2 overexpression, molecular lesions that do not prevent client loss but are nonetheless associated with reduced cell killing by 17-AAG. BIIB021 is also active in 17-AAG resistant cell lines (NIH-H69, MES SA Dx5, NCI-ADR-RES, Nalm6 and etc.). [4]

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
sf9 cells NWnJfVFoTnWwY4Tpc44h[XO|YYm= NYXLZYVGOyCq MUDCbY5lcW6pIHHm[olvcXS7IITvJIh2dWGwIF6teIVzdWmwYXygdI9tgUircz30ZYdo\WRiSGPQPVBj\XSjIDjEPUB1dyCHMkO2LUBmgHC{ZYPz[YQhcW5iaX7z[YN1KHOoOTDj[YxteyCjZoTldkA{KGi{czDifUBndHWxcnXzZ4Vv[2VicH;sZZJqgmG2aX;uJIF{e2G7LDDLbV01KG6P NF;mepQzPDN|MkS4PC=>
MCF7 cells Mlq1SpVv[3Srb36gZZN{[Xl? NVvrbZliUW6qaXLpeIlwdiCxZjDIV3A6OGGucHjhJIlvKGi3bXHuJG1ETjdiY3XscJMh[XO|ZYPz[YQh[XNiZHXndoFl[XSrb36gc4YhUGW{LUKsJGVEPTB;M{igcm0> M{fwdVIzQTN6MEOw
human BT474 cells NWXqTJZZTnWwY4Tpc44h[XO|YYm= MV;CbY5lcW6pIHHm[olvcXS7IITvJGh{eDlyIH71Z4xmd3SrZHWgZolv\GmwZzDkc41icW5iaX6gbJVu[W5iQmS0O|Qh[2WubIOsJGlEPTB;MD6xOEDPxE1? NIXXT3YzODZyOEezPC=>
NCI-H1299 cells NUDMdXhDTnWwY4Tpc44h[XO|YYm= MnPHNVIhcA>? NG\pU49T\WS3Y4Tpc44hcW5ib4j5[4VvKGOxboP1cZB1cW:wIILheIUhcW5iaIXtZY4hVkOLLVixNlk6KGOnbHzzJIlv[3WkYYTl[EBnd3JiMUKgbJJ{ M1jEbVI2Ozh|OUG1


体内試験 Oral administration of BIIB021 leads to tumor growth inhibition in many tumor xenograft models including N87, BT474, CWR22, U87, SKOV3 and Panc-1. [1] BIIB021 effectively inhibits growth of L540cy tumor at a dose of 120 mg/kg. [2] BIIB021 significantly enhances antitumor growth effect of radiation in JHU12 xenograft. [3]


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Hsp90 Binding Assay:

For fluorescence polarization competition measurements, the FITC-geldanamycin probe (20 nM) is reduced with 2 mM TCEP at room temperature for 3 hours, after which the solution is aliquoted and stored at -80 °C until used. Recombinant human Hsp90α (0.8 nM) and reduced FITC-geldanamycin (2 nM) are incubated in a 96-well microplate at room temperature for 3 hours in the presence of assay buffer containing 20 mM HEPES (pH 7.4), 50 mM KCl, 5 mM MgCl2, 20 mM Na2MoO4, 2 mM DTT, 0.1 mg/mL BGG, and 0.1% (v/v) CHAPS. Following this preincubation, BIIB021 in 100% DMSO is then added to final concentrations of 0.2 nM to 10 μM (final volume 100 μL, 2% DMSO). The reaction is incubated for 16 hours at room temperature and fluorescence is then measured in an Analyst plate reader, excitation = 485 nm, emission = 535 nm. High and low controls contained no BIIB021 or no Hsp90, respectively. The data are fit to a four-parameter curve and IC50 is generated.
細胞試験: [1]
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  • 細胞株: BT474, MCF-7, N87, HT29, H1650, H1299, H69 and H82 cells
  • 濃度: 3 nM - 1 μM
  • 反応時間: 5 days
  • 実験の流れ: A modified tetrazolium salt assay is used to measure the IC50. Tumor cells are added to 96-well plates and propagated for 24 hours before BIIB021 addition. BIIB021 is added to the plated cells. DMSO (0.03-0.003%) is included as a vehicle control. After incubation phenazine methosulfate (stock concentration 1 mg/mL) and 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium, inner salt (stock concentration 2 mg/mL) are mixed at a ratio of 1:20 and added to each well of a 96-well plate. Reduction of 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium, inner salt gives rise to a soluble formazan product that is secreted into the culture medium. After 4 hours incubation, the formazan product is quantitated spectrophotometrically at a wavelength of 490 nm. Data are acquired using SOFTmaxPRO software, and 100% viability is defined as the A490 of DMSO-treated cells stained with 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium, inner salt (the mean A490 of cells treated with DMSO at a range of 0.03-0.003%). Percent viability of each sample is calculated from the A490 values as follows: % viability = (A490 nm sample / A490 nm DMSO-treated cells × 100). The IC50 is defined as the concentration that gives rise to 50% inhibition of cell viabilit
+ 展開
  • 動物モデル: N87, BT474, CWR22, U87, SKOV3 and Panc-1 tumor models in BALB/c and athymic mice
  • 製剤: Phospho-lipon/sucrose emulsion [2]
  • 投薬量: 31, 62.5, and 125 mg/kg
  • 投与方法: Orally administered once daily

溶解度 (25°C)

体外 DMSO 64 mg/mL (200.77 mM)
Ethanol 2 mg/mL (6.27 mM)
Water 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):
30% propylene glycol, 5% Tween 80, 65% D5W
30 mg/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。


分子量 318.76


CAS No. 848695-25-0
in solvent
別名 CNF2024





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


  • 質量





開始濃度 x 開始体積 = 最終濃度 x 最終体積


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

  • C1



  • 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):




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


質量 濃度 体積 分子量


NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01017198 Completed Advanced Solid Tumors Biogen November 2009 Phase 1
NCT01004081 Completed Breast Cancer Biogen November 2009 Phase 2
NCT00618735 Completed Advanced Solid Tumors Biogen February 2008 Phase 1
NCT00618319 Completed GIST Biogen February 2008 Phase 2
NCT00412412 Completed Breast Cancer Biogen December 2007 Phase 1
NCT00344786 Terminated B-Cell Chronic Lymphocytic Leukemia Biogen February 2006 Phase 1



Handling Instructions


  • * 必須

HSP (e.g. HSP90)シグナル伝達経路

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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