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Enzalutamide [915087-33-1]

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Référence NB-64-30476-500mg

Conditionnement : 500mg

Marque : Neo Biotech

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Enzalutamide

(Synonyms: MDV3100) Copy Product Info

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Synonyms: MDV3100

Catalog No. T6002 Copy Product Info

Purity: 99.93%

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Enzalutamide (MDV3100) is an androgen receptor (AR) antagonist (IC50=36 nM in LNCaP) that activates autophagy, exhibits antitumor activity, and is commonly used in treating desmoplasia-resistant prostate cancer.

Cas No. 915087-33-1

With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.

For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.93%

Color:White

Product Introduction

Bioactivity

Description	Enzalutamide (MDV3100) is an androgen receptor (AR) antagonist (IC50=36 nM in LNCaP) that activates autophagy, exhibits antitumor activity, and is commonly used in treating desmoplasia-resistant prostate cancer.
Targets & IC50	SJSA-1:34.7 μM (LD50), Androgen receptor:36 nM (LNCaP cells), LNCaP cells:12 μM (LD50), PC3 cells:12 μM (LD50)
In vitro	METHODS: Human prostate cancer cells LNCaP, PC3 and human osteosarcoma cells SJSA-1 were treated with Enzalutamide (0.01-100 μM) for 1 h. Cell viability was measured using MTT. RESULTS: Enzalutamide was shown to decrease the viability of all cell lines, with LD50s of 12 μM, 23.4 μM, and 34.7 μM for LNCaP, PC3, and SJSA-1 cell lines, respectively. [1] METHODS: Human prostate cancer cells VCaP were treated with Enzalutamide (10 μM) for 1-3 days, and the expression levels of target proteins were detected by Western Blot. RESULTS: Enzalutamide up-regulated cleaved-PARP expression and induced apoptosis in human prostate cancer cells. [2]
In vivo	METHODS: To assay antitumor activity in vivo, Enzalutamide (1-50 mg/kg) was administered by gavage once daily for twenty-eight days to CB17SCID mice bearing human desmoplastic resistance tumor (CRPC) LNCaP-AR-Lux. RESULTS: Enzalutamide induced regression of tumor volume in a CRPC xenograft model and apoptosis in AR overexpanded prostate cancer cells. [3] METHODS: To assess the role of AR in bone metabolism and bone growth after sexual maturation, Enzalutamide (10-100 mg/kg, 1% carboxymethyl cellulose+0.5% Tween 80+5% dimethylsulfoxide) was administered orally to C57BL/6N mice once daily for twenty-one days. RESULTS: Enzalutamide decreased the amount of bone in the axial skeleton, and Enzalutamide significantly reduced the mechanical strength of the axial skeleton. After sexual maturity, Enzalutamide reduced bone mass in the axial skeleton but not in the appendicular skeleton of male mice. [4]
Synonyms	MDV3100
Cell Research	For in vitro experiments, LNCaP or LNCaP/AR cells (10^4 cells/well) were androgen-starved by growth in media containing 5-10% charcoal-stripped serum for 3-5 days. Then the cells were challenged with various concentrations of R1881, bicalutamide, RD162 or MDV3100 in media containing 5-10% charcoal-stripped serum [1].
Animal Research	In vivo tumorigenicity experiments were done by subcutaneous injection of 10^6 cells (100 uL in 50% Matrigel and 50% growth media) into the flanks of castrated male SCID mice. Daily gavage treatment (using a formulation of 1% carboxymethyl cellulose, 0.1% Tween-80, 5% DMSO) was initiated when tumor size reached ~100 mm3. Tumor size was measured weekly in three dimensions (l x w x d) with calipers. For in vivo luciferase imaging, d-luciferin substrate (100 μL, 15 mg/mL) was injected intraperitoneally. After 5 minutes, mice were anesthetized using isofluorane and imaged using a cooled charged-coupled device IVIS camera. Data were analyzed using Living Image 2.30 software [1].

Chemical Properties

Molecular Weight	464.44
Formula	C₂₁H₁₆F₄N₄O₂S
Cas No.	915087-33-1
Smiles	S=C1N(C(C)(C)C(=O)N1C2=CC(C(F)(F)F)=C(C#N)C=C2)C3=CC(F)=C(C(NC)=O)C=C3
Relative Density.	1.49 g/cm3

Storage & Solubility Information

Storage

Store at low temperature Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 257 mg/mL (553.35 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 8.5 mg/mL (18.3 mM), Suspension.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.1531 mL	10.7657 mL	21.5313 mL	107.6565 mL
5 mM	0.4306 mL	2.1531 mL	4.3063 mL	21.5313 mL
10 mM	0.2153 mL	1.0766 mL	2.1531 mL	10.7657 mL
20 mM	0.1077 mL	0.5383 mL	1.0766 mL	5.3828 mL
50 mM	0.0431 mL	0.2153 mL	0.4306 mL	2.1531 mL
100 mM	0.0215 mL	0.1077 mL	0.2153 mL	1.0766 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 µL Tween 80 and mix well until fully clarified.

3) Add 450 µL Saline,PBS or ddH₂O and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

Keywords

prostateMDV-3100MDV 3100LNCaPInhibitorinhibitEnzalutamidecellAutophagyAndrogenReceptorAndrogen Receptor

Related Tags: Enzalutamide chemical structure | Enzalutamide in vivo | Enzalutamide in vitro | Enzalutamide formula | Enzalutamide molecular weight