Enzalutamide (MDV3100) 化学構造
分子量: 464.44

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製品説明

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製品の説明

生物活性

製品説明 Enzalutamide (MDV3100)は、36nMのIC50をもつアンドロゲン受容体(AR)敵対者です。
ターゲット Androgen-receptor
IC50 36 nM [1]
In vitro試験 Enzalutamide has greater affinity to AR than Bicalutamide does in a competition assay with 16β-[18F]fluoro-5α-DHT (18-FDHT) in castration-resistant LNCaP/AR cells (AR-overexpressing). While Enzalutamide shows no agonism in LNCaP/AR prostate cells. Enzalutamide antagonizes induction of prostate-specific antigen (PSA) and transmembrane serine protease 2 (TMPRSS2), combination with the synthetic androgen R1881 in parental LNCaP cells. Enzalutamide could inhibit the transcriptional activity of a mutant AR protein (W741C, mutation of Trp741 to Cys). [1] Enzalutamide also prevents nuclear translocation and co-activator recruitment of the ligand-receptor complex. [2]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
human LNCAP NVn5b4FSS3m2b4TvfIlkKEG|c3H5 MYe3JIRigXN? NEKyWXc6PSViRYTPTC=> MWrJR|UxRTVwMUKg{txO NFn1RnUzOzdzM{W2Oy=>
human LNCAP Ml\KSpVv[3Srb36gRZN{[Xl? MWixJO69VQ>? MoOxSG1UVw>? MXzJcohq[mm2czDwdo9{fGG2ZTDzdIVkcW[rYzDhcpRq\2WwIIPlZ5JmfGmxbjDpckBpfW2jbjDMUmNCWCClZXzsd{BmgHC{ZYPzbY5oKGGwZILv[4VvKHKnY3XweI9zKGG2IEGwNE0yODBybl2= NYn1[45FOjB{MUi3NVc>
VCaP MVTGeY5kfGmxbjDBd5NigQ>? NFHQN44yOCEQvF2= MnviNlQhcA>? MV;EUXNQ NGXmZ3hUfXCycnXzd4V{KGyrZ3Hu[E1u\WSrYYTl[EBCWi2ITDDzbYdv[Wyrbneg MVOyNlcyODR|Nh?=
BCK4 NFjNXmhHfW6ldHnvckBCe3OjeR?= M2O1Z|ExKM7:TR?= M2XJeVch\GG7cx?= NVuyfZV7TE2VTx?= NXXEdG5FUW6qaXLpeJMh\XO2cnHkbY9tNW2nZHnheIVlKHC{b3zp[oVz[XSrb36= NXruZ4pGOjR2NUGxNFk>
MCF7s MnjOSpVv[3Srb36gRZN{[Xl? M2DNNVExKM7:TR?= NHu2SYw3KGSjeYO= NV7PeGVDTE2VTx?= MkLSTY5pcWKrdIOg[ZN1emGmaX;sMY1m\GmjdHXkJJBzd2yrZnXyZZRqd25? MkTRNlQ1PTFzMEm=
PC-3 MYHGeY5kfGmxbjDBd5NigQ>? MXKxNEDPxE1? MlLnO|IhcA>? M4DiS2ROW09? M4PkV2Rw\XNibn;0JIlvcGmkaYSgZ4VtdCCycn;sbYZmemG2aX;u MViyOVM1PDh4NB?=
CWR22Rv1 MVvGeY5kfGmxbjDBd5NigQ>? M3G4PVE2KM7:TR?= M3jCWFI1KGh? NH:4NIdFVVOR MnnxSI9meyCwb4SgZYZn\WO2IITo[UBnfWyuIHzlcod1cCCDUjDlfJBz\XO|aX;u MVuyN|cyOzV4Nx?=

... Click to View More Cell Line Experimental Data

In vivo試験 Enzalutamide induces great tumor regression in castrate male mice bearing LNCaP/AR xenografts at a dose of 10 mg/kg. [1]
臨床試験 Enzalutamide is currently in Phase III clinical trial in progressive metastatic prostate cancer.
特集

プロトコル (参考用のみ)

キナーゼアッセイ: [3]

AR reporter assay Enzalutamide is evaluated by an artificial AR response reporter system in a hormone refractory prostate cancer cell line. In this system, the prostate cancer LNCaP cells are engineered to stably express about 5-fold higher level of AR than endogenous level. The exogenous AR has similar properties to endogenous AR in that both are stabilized by a synthetic androgen R1881. The AR-over expressed cells are also engineered to stably incorporate an AR response reporter and the reporter activity of these cells shows features of hormone refractory prostate cancer. The antagonistic activity of Enzalutamide is tested in the presence of 100 pM of R1881. Engineered LNCaP cells are maintained in Iscove's medium containing 10% fetal bovine serum (FBS). Two days prior to Enzalutamide treatment, the cells are grown in Iscove's medium containing 10% charcoal-stripped FBS (CS-FBS) to deprive of androgens. The cells are split and grown in Iscove's medium containing 10% CS-FBS with 100 pM of R1881 and increasing concentrations of Enzalutamide. After two days of incubation, reporter activities are assayed.

細胞アッセイ: [1]

細胞株 LNCaP or LNCaP/AR cells
濃度 0-10 μM
反応時間 1-4 days
実験の流れ Enzalutamide is diluted in DMSO. LNCaP or LNCaP/AR cells (104 cells/well) are androgen-starved by growth in media containing 5-10% charcoal-stripped serum for 3-5 days. Then the cells are challenged with various concentrations of Enzalutamide in media containing 5-10% charcoal-stripped serum.

動物実験: [1]

動物モデル Castration-resistant LNCaP/HR xenografts in male SCID mice
製剤 Formulated in 1% carboxymethyl cellulose, 0.1% Tween-80, 5% DMSO
投薬量 10 mg/kg
投与方法 Administered via gavage daily

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download Enzalutamide (MDV3100) SDF
分子量 464.44
化学式

C21H16F4N4O2S

CAS No. 915087-33-1
保管 2年-20℃
6月-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 92 mg/mL warming (198.08 mM)
<1 mg/mL (<1 mM)
エタノール <1 mg/mL (<1 mM)
In vivo 2% DMSO+30% PEG300 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.
化学名  4-​[3-​[4-​cyano-​3-​(trifluoromethyl)​phenyl]​-​5,​5-​dimethyl-​4-​oxo-​2-​thioxo-​1-​imidazolidinyl]​-​2-​fluoro-​N-​methyl-benzamide

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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