MDV3100 Inhibitor CAS No. 915087-33-1

Cat. No.	Name	Size	Price
KI0325	MDV3100	5 mg	$259.2
	MDV3100	10 mg	$460
	MDV3100	50 mg	$1404

Chemical Characteristic

Product Name	MDV3100
Synonyms	Enzalutamide
CAS No.	915087-33-1
Molecular Weight	464.44
Formula	C₂₁H₁₆F₄N₄O₂S
Chemical Name	4-[3-[4-Cyano-3-(trifluoromethyl)phenyl]-5,5-dimethyl-4-oxo-2-thioxo-1-imidazolidinyl]-2-fluoro-N-methylbenzamide
Smiles	C(=O)(c1c(cc(cc1)N1C(=S)N(C(=O)C1(C)C)c1cc(c(cc1)C#N)C(F)(F)F)F)NC
Chemical Structure
Documents	HPLC MS COA

Biological activities

MDV3100 is an androgen receptor (AR) antagonist with an IC50 of 36 nM. MDV3100 blocks AR binding, nuclear translocation, and co-activator recruitment. ^[1] MDV3100 binds AR with 8-fold higher affinity compared to bicalutamide. And MDV3100 does not activate either wild-type AR, or the T877A or W741C mutants. In two AR over expressing cell lines, LNCaP/AR and VCaP, MDV3100 inhibits AR-mediated transcription and cell growth in vitro while bicalutamide does not. When bound to MDV3100 rather than bicalutamide, AR translocates into the nucleus far less efficiently and a significant AR fraction remains in the cytosol.^[2] MDV3100 retains activity in the setting of increased androgen receptor expression. Both RD162 and MDV3100 bind to the androgen receptor with greater relative affinity than bicalutamide, reduce the efficiency of its nuclear translocation and impair both DNA binding to androgen response elements and recruitment of coactivators. MDV3100 also induces tumor regression in mouse models of castration-resistant human prostate cancer. MDV3100 antagonizes induction of PSA and TMPRSS2 by the synthetic androgen R1881 in parental LNCaP cells. In the human prostate cancer cell line VCaP which has endogenous AR gene amplification, MDV3100 suppresses growth. In addition, MDV3100 inhibits the transcriptional activity of a mutant AR protein (W741C) isolated from a patient with acquired resistance to bicalutamide.^[1] MDV3100 induces tumor regression in established LNCaP/AR xenograft tumors growing in castrate male mice, while bicalutamide treatment merely slows tumor growth compared to vehicle-treated controls. ^[2]

Protocols

MDV3100 is dissolved in 1% carboxymethyl cellulose, 0.1% Tween-80 and 5% DMSO as stock solution. ^[1]

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] Chen Y, et al. Anti-androgens and androgen-depletingtherapies in prostatecancer: new agents for an establishedtarget. Lancet Oncol. 2009, 10(10): 981-991. [3] Watson PA, et al. Constitutively active androgen receptor splice variants expressed in castration-resistant prostate cancer require full-length androgen receptor. Proc Natl Acad Sci U S A. 2010, 107(39): 16759-16765.

Please click here to fill online order form, and we will make sure to supply you product with detail information. This process usually takes between 24 to 48 hours, depending on products stock avaliability. All inquires and subsequent projects are handled in the strictest confidence and will be backed by a confidentiality agreement if required.

KareBay^TM provides scientists and clinicians with a wide range of biotechnological products and science lab supplies for chemical research and analyzing life processes. KareBay's extensive capabilities include commercializing reagents and kits, manufacturing biotech products and providing contract research services to organizations worldwide. Our many global labs, offices, and business partners enable KareBay to extend its products and services to its customer base around the world.

Our products are used for research, laboratory and further evaluation purposes. They are not for human use.

About

KareBay^TM Biochem
Sitemap
Blog

Custom Services