BIIB021

製品コードS1175 別名:CNF2024

BIIB021化学構造

分子量(MW):318.76

BIIB021は一種の経口有効で、全部人工合成の小分子HSP90阻害剤で、Ki値とEC50値が1.7nMと38nMに分かれることです。臨床2期。

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USD 151 あり
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カスタマーフィードバック(9)

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

    PLoS Pathog 2012 8(11), e1003048. 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.

製品安全説明書

HSP (e.g. HSP90)阻害剤の選択性比較

生物活性

製品説明 BIIB021は一種の経口有効で、全部人工合成の小分子HSP90阻害剤で、Ki値とEC50値が1.7nMと38nMに分かれることです。臨床2期。
ターゲット
HSP90 [1] HSP90 [1]
1.7 nM(Ki) 38 nM(EC50)
体外試験

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]

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]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[1]
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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]
+ 展開
  • 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
    (参考用のみ)
動物試験:[1]
+ 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
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 64 mg/mL (200.77 mM)
Ethanol 2 mg/mL (6.27 mM)
Water slightly soluble or insoluble
体内 順序で溶剤を入れること:
30% propylene glycol, 5% Tween 80, 65% D5W
30 mg/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 318.76
化学式

C14H15ClN6O

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

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
NCT01004081 Completed Breast Cancer Biogen November 2009 Phase 2
NCT01017198 Completed Advanced Solid Tumors Biogen November 2009 Phase 1
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

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

HSP (e.g. HSP90)信号経路図

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