MDV3100 free base · Synonyms: Enzalutamide

Enzalutamide is an androgen receptor antagonist.

For research use only. Not for human or veterinary use.

Target Androgen Receptor Autophagy

Research area Cancer

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Data Sheet SDS COA

MDV3100 structure

CAS No.: 915087-33-1

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
10 g	USD 398.00	BP-02101-10g	In stock	Get quote
20 g	USD 798.00	BP-02101-20g	In stock	Get quote
50 g	USD 1,480.00	BP-02101-50g	In stock	Get quote
100 g	USD 2,880.00	BP-02101-100g	In stock	Get quote
200 g	Inquire	BP-02101-200g	In stock	Inquire

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Description

Enzalutamide (MDV3100) is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells. Enzalutamide is an autophagy activator.

Biological activity

In Vitro Enzalutamide (MDV3100) has greater affinity to AR than ICI 176334 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 inhibits the transcriptional activity of a mutant AR protein (W741C, mutation of Trp741 to Cys). Enzalutamide also prevents nuclear translocation and co-activator recruitment of the ligand-receptor complex. In Vivo Enzalutamide (MDV3100) induces great tumor regression in castrate male mice bearing LNCaP/AR xenografts at a dose of 10 mg/kg. Enzalutamide shows dose-independent pharmacokinetics at intravenous and oral doses of 0.5-5 mg/kg.

Identifiers

SMILES: CNC(=O)C1=CC=C(C=C1F)N1C(=S)N(C(=O)C1(C)C)C1=CC=C(C#N)C(=C1)C(F)(F)F
InChIKey: WXCXUHSOUPDCQV-UHFFFAOYSA-N

Specifications

MW (average): 464.4360
Formula: C₂₁H₁₆F₄N₄O₂S
CAS No.: 915087-33-1
Physical state: Solid
Color: White to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

In vitro: DMSO : ≥ 50 mg/mL

Documents

References

[1]. Tran C, et al. Development of a second-generation antiandrogen for treatment of advanced prostate cancer. Science, 2009, 324 (5928), 787-790.

[2]. Scher HI, et al. Antitumour activity of MDV3100 in castration-resistant prostate cancer: a phase 1-2 study. Lancet, 2010, 375(9724), 1437-1446.

[3]. Guerrero J, et al. Enzalutamide, an androgen receptor signaling inhibitor, induces tumor regression in a mouse model of castration-resistant prostate cancer. Prostate. 2013 Sep;73(12):1291-305.

[4]. Kim TH, et al. Pharmacokinetics of enzalutamide, an anti-prostate cancer drug, in rats. Arch Pharm Res. 2015 Nov;38(11):2076-82.

Same target

Search Androgen Receptor

Same research area

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