Date published: 2026-3-17

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MDV3100 (CAS 915087-33-1)

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Alternate Names:
MDV3100 is also known as Enzalutamide.
Application:
MDV3100 is a non-steroidal androgen receptor inhibitor, applied against advanced cancers that depend on androgen receptor signaling.
CAS Number:
915087-33-1
Purity:
≥98%
Molecular Weight:
464.44
Molecular Formula:
C21H16F4N4O2S
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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MDV3100 is an androgen receptor inhibitor and antagonizes induction of prostate-specific antigen (PSA) and transmembrane serine protease 2 (TMPRSS2) in combination with the synthetic androgen R1881 in parental LNCaP cells. It also prevents nuclear translocation and co-activator recruitment of the ligand-receptor complex. It reduces the efficiency of nuclear translocation of the androgen receptor, and then impairs its binding to DNA and the recruitment of coactivators. MDV3100 is able to induce tumor regression in mice models of prostate cancer.


MDV3100 (CAS 915087-33-1) References

  1. [Strategies in castration-resistant prostate cancer].  |  Bessede, T., et al. 2011. Prog Urol. 21 Suppl 2: S68-71. PMID: 21397833
  2. A novel antiandrogen, Compound 30, suppresses castration-resistant and MDV3100-resistant prostate cancer growth in vitro and in vivo.  |  Kuruma, H., et al. 2013. Mol Cancer Ther. 12: 567-76. PMID: 23493310
  3. Methylselenol prodrug enhances MDV3100 efficacy for treatment of castration-resistant prostate cancer.  |  Zhan, Y., et al. 2013. Int J Cancer. 133: 2225-33. PMID: 23575870
  4. Cotargeting Androgen Receptor and Clusterin Delays Castrate-Resistant Prostate Cancer Progression by Inhibiting Adaptive Stress Response and AR Stability.  |  Matsumoto, H., et al. 2013. Cancer Res. 73: 5206-17. PMID: 23786771
  5. An F876L mutation in androgen receptor confers genetic and phenotypic resistance to MDV3100 (enzalutamide).  |  Korpal, M., et al. 2013. Cancer Discov. 3: 1030-43. PMID: 23842682
  6. Anti-androgen receptor ASC-J9 versus anti-androgens MDV3100 (Enzalutamide) or Casodex (Bicalutamide) leads to opposite effects on prostate cancer metastasis via differential modulation of macrophage infiltration and STAT3-CCL2 signaling.  |  Lin, TH., et al. 2013. Cell Death Dis. 4: e764. PMID: 23928703
  7. Antitumour activity of enzalutamide (MDV3100) in patients with metastatic castration-resistant prostate cancer (CRPC) pre-treated with docetaxel and abiraterone.  |  Bianchini, D., et al. 2014. Eur J Cancer. 50: 78-84. PMID: 24074764
  8. Androgen receptor gene mutation, rearrangement, polymorphism.  |  Eisermann, K., et al. 2013. Transl Androl Urol. 2: 137-147. PMID: 25045626
  9. What is the next generation therapeutic strategy for castration-resistant prostate cancer.  |  Wen, SM., et al. 2015. Asian J Androl. 17: 223-4. PMID: 25432503
  10. Ailanthone targets p23 to overcome MDV3100 resistance in castration-resistant prostate cancer.  |  He, Y., et al. 2016. Nat Commun. 7: 13122. PMID: 27959342
  11. Characterization of a novel p110β-specific inhibitor BL140 that overcomes MDV3100-resistance in castration-resistant prostate cancer cells.  |  He, C., et al. 2017. Prostate. 77: 1187-1198. PMID: 28631436
  12. Blocking the Feedback Loop between Neuroendocrine Differentiation and Macrophages Improves the Therapeutic Effects of Enzalutamide (MDV3100) on Prostate Cancer.  |  Wang, C., et al. 2018. Clin Cancer Res. 24: 708-723. PMID: 29191973
  13. Abiraterone and MDV3100 inhibits the proliferation and promotes the apoptosis of prostate cancer cells through mitophagy.  |  Han, J., et al. 2019. Cancer Cell Int. 19: 332. PMID: 31827406
  14. Enhanced antitumor efficacy by combining afatinib with MDV3100 in castration-resistant prostate cancer.  |  Li, J., et al. 2022. Pharmazie. 77: 59-66. PMID: 35209965

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

MDV3100, 5 mg

sc-364354
5 mg
$245.00

MDV3100, 50 mg

sc-364354A
50 mg
$1051.00