Apalutamide (ARN-509)


Apalutamide (ARN-509)化学構造


Apalutamide (ARN-509) is a selective androgen receptor inhibitor with IC50 of 16 nM.

サイズ 価格(税別) 在庫  
JPY 66400.00 あり
JPY 34860.00 あり
JPY 44820.00 あり
JPY 161020.00 あり


  • ONC1-0013B inhibits AR activity in vitro. A. ONC1-0013B structure. B. LnCAP cells cultured (10% CSS) for 3 days, then treated with tested compounds in presence of 1nM DHT for 1 day. PSA expression plotted as percentage of vehicle control (DMSO; n=2, mean±SEM). Ki values: 20.0±5.5nM (ONC1-13B), 30.8±7.7nM (MDV3100), 38.4nM (ARN-509). Mean±SEM from 5 replicate experiments (except ARN-509). C. LnCAP cells cultured (10% CSS) for 3 days, then treated with tested compounds in presence of 1nM DHT for 5 days. Viable cells plotted as percentage of vehicle control (DMSO; n=2, mean±SEM). IC50 values: 30nM (ONC1-13B), 148nM (MDV3100), 240nM (ARN-509). D. Competitive-binding assay vs AR ligand Fluormone™ (PolarScreen™ Androgen Receptor Competitor Assay). IC50 values: 19nM (DHT), 7.9uM (ONC1-13B), 16.3uM (MDV3100).

    J Cancer, 2014, 5(2):133-42.. Apalutamide (ARN-509) purchased from Selleck.


Androgen Receptor阻害剤の選択性比較


製品説明 Apalutamide (ARN-509) is a selective androgen receptor inhibitor with IC50 of 16 nM.
Androgen Receptor [1]
(Cell-free assay)
16 nM

ARN-509 (< 10 μM) inhibits androgen-mediated induction or repression of mRNA expression levels for 13 endogenous genes including PSA and TMPRSS2 in the LNCaP/AR prostate cancer cell line. ARN-509 (< 10 μM) inhibits the proliferative effect of R1881 (30 pM) in the LNCaP/AR prostate cancer cell line. ARN-509 (10 μM) impairs AR nuclear localization and thus reduces the concentration of AR available to bind androgen response elements (ARE) in LNCaP cells expressing AR-EYFP. ARN-509 (10 μM) is able to effectively compete with R1881 (1 nM) and prevent AR from binding to promoter regions. ARN-509 inhibits R1881-induced VP16-AR–mediated transcription with IC50 of 0.2 μM in Hep-G2 cells expressing a VP16-AR fusion protein and an ARE-driven luciferase reporter. [1]

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
LNCAP cells M4L6UXBzd2yrZnXyZZRqd25iYYPzZZk> MV[zJIRigXN? MX;BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEyQQ1HQJINmdGy|IHHmeIVzKDNiZHH5d{whUUN3ME2wMlE4PCEQvF2= MoT0NlYxPDZ|MUO=
PSN1 cells M3[wVGN6fG:2b4jpZ4l1gSCjc4PhfS=> NVTSWotIQTZiaB?= MlTWR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gVHNPOSClZXzsd{Bi\nSncjC5OkBpenNiYomgRXRRNWyrdHWgcJVucW6nc3PlcoNmKGG|c3H5MEBKSzVyPUCuNFYh|ryP MU[yNlI1Pzd6OB?=
PSN1 cells MorKSpVv[3Srb36gZZN{[Xl? MoDXN|Ahdk1? MXOyOEBp MXHJcoR2[3Srb36gc4Yh[2WubDDjfYNt\SCjcoLld5QhcW5iaIXtZY4hWFOQMTDj[YxteyCjc4Pld5Nm\CCjczDhZ4N2dXWuYYTpc44h[XRiR{KvUUBxcGG|ZTDj[YxteyCjdDCzNEBvVSCjZoTldkAzPCCqcoOgZpkh\myxdzDjfZRwdWW2com= MVyyNlI1Pzd6OB?=


体内試験 ARN-509 (10 mg/kg/d, oral) inhibits tumor growth with decreased proliferative index and increased apoptotic rate in castrate male immunodeficient mice harboring LNCaP/AR-luc xenograft tumors. ARN-509 dose dependently inhibits tumor growth with highest efficacy at dose of 30 mg/kg/day in castrate male immunodeficient mice harboring LNCaP/AR-luc xenograft tumors. ARN-509 dosed at 10 mg/kg/d for 28 days results in a 3-fold reduction in prostates weight associated with lacking glandular secretory activity and 1.7-fold reduction in epididymis weight in adult male dogs. ARN-509 (10 mg/kg/d, oral) inhibits cell proliferation of prostate tissues in adult male dogs. [1] ARN-509 is safe and well tolerated in 24 patients with metastatic CRPC who has progressed on prior treatments and peak plasma concentrations occurred 2 to 3 hours after administration. ARN-509 results in durable PSA declines at doses ranging from 30 to 300 mg in patients with metastatic CRPC. [2] ARN-509 shows powerful anti-cancer activity and induces durable remissions long after therapy completion in castrate resistant prostate cancer mouse models. [3]


細胞試験: [1]
+ 展開
  • 細胞株: LNCaP/AR prostate cancer cell line
  • 濃度: 10 μM
  • 反応時間: 48 hours
  • 実験の流れ: Cells are incubated for 48 hours, after which ARN-509 is added in a 16 μL volume to the RPMI culture medium. For the antagonist mode assay, the ARN-509 is diluted in culture medium also containing 30 pM R1881. After 7 days' incubation, 16 μL of CellTiter-Glo Luminescent Cell Viability Assay is added and Relative Luminescence Units (RLUs) measured.
+ 展開
  • 動物モデル: Castrate male immunodeficient mice harboring LNCaP/AR-luc xenograft tumors
  • 製剤: 15% Vitamin E-TPGS and 65% of a 0.5% w/v CMC solution in 20 mM citrate buffer (pH 4.0)
  • 投薬量: 30 mg/kg/day
  • 投与方法: Orally

溶解度 (25°C)

体外 DMSO 18 mg/mL (37.7 mM)
Ethanol 5 mg/mL (10.47 mM)
Water Insoluble
体内 順序で溶剤を入れること:
0.5% CMC, pH4.0
14 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。


分子量 477.43


CAS No. 956104-40-8
別名 N/A





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


  • マス




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


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

  • 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


マス 濃度 ボリューム 分子量


NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02949284 Not yet recruiting Stage II Prostate Adenocarcinoma|Stage III Prostate Adenocarcinoma Rutgers, The State University of New Jersey|National Cancer Institute (NCI) June 2017 Phase 2
NCT02721979 Not yet recruiting Stage II Prostate Adenocarcinoma University of Washington|National Cancer Institute (NCI) December 2016 Phase 2
NCT02770391 Recruiting Prostate Cancer Case Comprehensive Cancer Center October 2016 Phase 2
NCT02849990 Not yet recruiting Stage III Prostate Adenocarcinoma|Stage III Prostate Cancer|Stage IV Prostate Adenocarcinoma|Stage IV Prostate Cancer University of Washington|National Cancer Institute (NCI)|Janssen Scientific Affairs, LLC October 2016 Phase 2
NCT02772588 Recruiting Prostate Cancer Memorial Sloan Kettering Cancer Center|Janssen Pharmaceuticals|Weill Medical College of Cornell University|University of Michigan May 2016 Phase 2
NCT02703623 Recruiting Prostate Cancer M.D. Anderson Cancer Center|Bristol-Myers Squibb|Janssen, LP|Sanofi May 2016 Phase 2



Handling Instructions


  • * 必須

Androgen Receptor信号経路図

相関Androgen Receptor製品

Tags: Apalutamide (ARN-509)を買う | Apalutamide (ARN-509) ic50 | Apalutamide (ARN-509)供給者 | Apalutamide (ARN-509)を購入する | Apalutamide (ARN-509)費用 | Apalutamide (ARN-509)生産者 | オーダーApalutamide (ARN-509) | Apalutamide (ARN-509)化学構造 | Apalutamide (ARN-509)分子量 | Apalutamide (ARN-509)代理店
細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID