Darolutamide (ODM-201)

製品コードS7559 バッチS755903

印刷

化学情報

Chemical Structure Synonyms BAY-1841788 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C19H19ClN6O2
分子量 398.85 CAS No. 1297538-32-9
Solubility (25°C)* 体外 DMSO 80 mg/mL (200.57 mM)
Ethanol (warmed with 50ºC water bath) 4 mg/mL (10.02 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Darolutamide (ODM-201, BAY-1841788) is a novel androgen receptor (AR) antagonist that blocks AR nuclear translocation with Ki of 11 nM. Phase 3.
in vitro In AR-HEK293 cells stably expressing full-length hAR, this compound inhibits human AR (hAR) with IC50 of 26 nM. It also inhibits VCaP cell proliferation with IC50 of 230 nM, while having no effect on the viability of AR-negative cell lines tested, DU-145 prostate cancer cells and H1581 lung cancer cells. [1]
in vivo In mice bearing VCaP xenografts, it (50 mg/kg, p.o.) significantly inhibits castration-resistant prostate tumor growth. [1]

プロトコル(参考用のみ)

キナーゼアッセイ AR binding affinity
AR binding affinities of test compounds are studied in cytosolic lysates obtained from ventral prostates of castrated rats by a competition binding assay. Fresh prostates are minced and homogenized with Buffer A containing protease inhibitors. The homogenates are centrifuged and the resultant supernatants are treated with a dextran-coated charcoal solution to remove endogenous steroids. The dissociation constant of the radio ligand [3H]mibolerone for isolated rat ARs is determined in a saturation binding experiment. For the determination of Ki values, prostate cytosol preparations and 1 nM [3H]mibolerone are incubated with increasing concentrations of this compound overnight. After the incubation, bound and free steroids are separated by treatment with 100 μL of dextran-coated charcoal suspension. Bound radioactivity is determined by counting 100 μL of supernatant fraction in 200 μL of scintillation fluid using a microbeta counter. All procedures are carried out at 0–4 °C.
細胞アッセイ 細胞株 DU-145, H1581, and VCaP cells
濃度 ~10 μM
反応時間 4 days
実験の流れ VCaP cells are treated with a submaximal concentration of mibolerone (0.1 nM) and increasing concentrations of test compounds in steroid-free assay medium supplemented with 4 mM GlutaMAX. After a 4-day incubation with the compounds, cell viability is measured using a WST-1 cell proliferation assay. To rule out non-AR –mediated toxicity, AR-negative PC cells (DU-145) and lung cancer cells (H1581) are treated with an increasing concentration of Darolutamide (ODM-201), and cell viability is measured as described above.
動物実験 動物モデル BALB/c nude male mice bearing VCaP xenografts
投薬量 50 mg/kg, bid
投与方法 p.o.

参考

  • https://pubmed.ncbi.nlm.nih.gov/26137992/

カスタマーフィードバック

Data from [Data independently produced by , , Clin Cancer Res, 2018, doi:10.1158/1078-0432.CCR-18-1469]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Engineering bi-directional chemically-modulated synthetic condensates for cellular control [ Nat Commun, 2025, 16(1):6587] PubMed: 40675979
Clinical Context Shapes the Relationship Between Genomic Alterations and Response to AR Inhibitors and Chemotherapy in Metastatic Prostate Cancer [ Clin Cancer Res, 2025, 10.1158/1078-0432.CCR-24-1812] PubMed: 40227200
BCL2 drives castration resistance in castration-sensitive prostate cancer by orchestrating reciprocal crosstalk between oncogenic pathways [ Cell Rep, 2025, 44(6):115779] PubMed: 40448998
Cholesterol metabolism regulated by CAMKK2-CREB signaling promotes castration-resistant prostate cancer [ Cell Rep, 2025, 44(6):115792] PubMed: 40483692
Increased translation driven by non-canonical EZH2 creates a synthetic vulnerability in enzalutamide-resistant prostate cancer [ Nat Commun, 2024, 15(1):9755] PubMed: 39567499
Darolutamide-mediated phospholipid remodeling induces ferroptosis through the SREBP1-FASN axis in prostate cancer [ Int J Biol Sci, 2024, 20(12):4635-4653] PubMed: 39309439
Patient-derived rhabdomyosarcoma cells recapitulate the genetic and transcriptomic landscapes of primary tumors [ iScience, 2024, 27(10):110862] PubMed: 39319271
Loss of LCMT1 and biased protein phosphatase 2A heterotrimerization drive prostate cancer progression and therapy resistance [ Nat Commun, 2023, 14(1):5253] PubMed: 37644036
Loss of LCMT1 and biased protein phosphatase 2A heterotrimerization drive prostate cancer progression and therapy resistance [ Nat Commun, 2023, 14(1):5253] PubMed: 37644036
Pharmacological Targeting of Androgen Receptor Elicits Context-Specific Effects in Estrogen Receptor-Positive Breast Cancer [ Cancer Res, 2023, 83(3):456-470] PubMed: 36469363

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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