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Darolutamide (Synonyms: ODM-201; BAY-1841788)

製品番号: HY-16985 純度: 99.03%
取扱説明書

Darolutamide (ODM-201;BAY-1841788) is a potent androgen receptor (AR) antagonist with an IC50 of 26 nM in in vitro assay.

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Darolutamide 構造式

Darolutamide 構造式

CAS 番号 : 1297538-32-9

容量 価格(税別) 在庫状況 数量
無料サンプル (0.5-1 mg)   今すぐ申し込む  
10 mM * 1  mL in DMSO USD 132 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 120 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 190 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 450 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 850 在庫あり
Estimated Time of Arrival: December 31
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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製品説明

Darolutamide (ODM-201;BAY-1841788) is a potent androgen receptor (AR) antagonist with an IC50 of 26 nM in in vitro assay.

IC50 & Target

IC50: 26 nM (AR-HEK293 cells, AR)[1]

体外実験

In competitive AR binding assays, the inhibition constant (Ki) values of Darolutamide (ODM-201) are 11 nM. ODM-201and ORM-15341 suppresse androgen-induced cell proliferation more efficaciously than enzalutamide or ARN-509, IC50 values being 230 and 170 nM for Darolutamide and ORM-15341 vs. 410 and 420 nM for enzalutamide and ARN-509. Darolutamide has no effect on the viability of AR-negative cell lines tested, DU-145 prostate cancer cells and H1581 lung cancer cells confirming that the antiproliferative properties of Darolutamide and ORM-15341 are specific to AR-dependent PC cells[1].

体内実験

Darolutamide (ODM-201) showes a significant antitumor activity with both doses, 50 mg/kg twice daily being more efficacious compared to castrated, untreated mice (p<0.001) or Enzalutamide (p=0.0245), which also showes inhibition of tumor growth (p<0.05) vs. castrated, untreated mice. Further, there is no sign of treatment-related toxicities; the body weights of mice treated with Darolutamide twice daily do not decrease significantly during the treatment[1].

臨床実験
分子量

398.85

分子式

C₁₉H₁₉ClN₆O₂

CAS 番号

1297538-32-9

SMILES

ClC1=C(C#N)C=CC(C2=NN(C[[email protected]](C)NC(C3=NNC(C(O)C)=C3)=O)C=C2)=C1

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 100 mg/mL (250.72 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5072 mL 12.5360 mL 25.0721 mL
5 mM 0.5014 mL 2.5072 mL 5.0144 mL
10 mM 0.2507 mL 1.2536 mL 2.5072 mL
*Please refer to the solubility information to select the appropriate solvent.
体内:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.27 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.27 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.27 mM); Clear solution

*All of the co-solvents are provided by MCE.
参考文献
細胞実験
[1]

To study the antiproliferative properties of Darolutamide and ORM-15341, the VCaP cell line originally derived from a bone metastasis of a CRPC patient is used. The VCaP cell line is characterized with endogenous AR gene amplification and AR overexpression30, typical for CRPC. VCaP cells are cultured in RPMI-1640 medium and supplemented with 10% fetal bovine serum (FBS), 100 UI/mL penicillin, 100 μ g/mL streptomycin, and 4 mM VCaP[1].

MCE はこれらの方法の精度を確認していません。 こちらは参照専用です。

動物実験
[1]

To elucidate the in vivo efficacy of Darolutamide in a CRPC mouse model, castrated male nude mice with subcutaneously injected VCaP cells are treated orally with ODM-201 (50 mg/kg) once (qd) or twice daily (bid), or with enzalutamide (20 mg/kg, qd) for 37 days. The dose for enzalutamide is selected based on previously published studies9 and our pharmacokinetic (PK) analyses which reveales that in mice the systemic exposure (AUC0–24) for this dose of enzalutamide is 2.5 times higher than that for Darolutamide (50 mg/kg, bid). Moreover, enzalutamide exhibited a long plasma half-life (18.3 hours) while the half-life of Darolutamide in mice is not optimal (1.6 hours) supporting once daily dosing for enzalutamide and higher dose and more frequent dosing for ODM-201[1].

MCE はこれらの方法の精度を確認していません。 こちらは参照専用です。

参考文献
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Keywords:

DarolutamideODM-201BAY-1841788ODM201ODM 201BAY1841788BAY 1841788Androgen ReceptorInhibitorinhibitorinhibit

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製品名:
Darolutamide
製品番号:
HY-16985
数量:
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