ODM-201 (Darolutamide)

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 4 mg/mL (10.02 mM)
Water Insoluble
* <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)は、アンドロゲン受容体(AR)の核内移行をKi11 nMで阻害する新規ARアンタゴニストである。第3相。
in vitro In AR-HEK293 cells stably expressing full-length hAR, Darolutamide (ODM-201) inhibits human AR (hAR) with IC50 of 26 nM. It inhibits VCaP cell proliferation with IC50 of 230 nM, while has no effect on the viability of AR-negative cell lines tested, DU-145 prostate cancer cells and H1581 lung cancer cells.
in vivo In mice bearing VCaP xenografts, Darolutamide (ODM-201) (50 mg/kg, p.o.) significantly inhibits castration-resistant prostate tumor growth.

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, including Darolutamide (ODM-201), 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 test compounds 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
Pharmacological Targeting of Androgen Receptor Elicits Context-Specific Effects in Estrogen Receptor-Positive Breast Cancer [ Cancer Res, 2023, 83(3):456-470] PubMed: 36469363
Allosteric inhibition of HSP70 in collaboration with STUB1 augments enzalutamide efficacy in antiandrogen resistant prostate tumor and patient-derived models [ Pharmacol Res, 2023, 189:106692] PubMed: 36773708

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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