Prinaberel


Catalog No. size PriceQuantity
M6942-2 2mg solid $136
M6942-10 10mg solid $563

Description

Cas:524684-52-4

Product Information:

Prinaberel, also known as ERB-041, is a drug which acts as a highly selective agonist of the ERβ subtype of the estrogen receptor. It is used in scientific research to elucidate the role of the ERβ receptor. Studies have indicated that selective ERβ agonists like prinaberel could be useful in the clinical treatment of a variety of medical conditions including inflammatory bowel disease, rheumatoid arthritis, endometriosis, and sepsis. Accordingly, prinaberel either was or still is under investigation by Wyeth for the treatment of some of these conditions.

 

Chemical Formula: C15H10FNO3

 

Exact Mass: 271.06447

 

Molecular Weight: 271.24

 

Elemental Analysis: C, 66.42; H, 3.72; F, 7.00; N, 5.16; O, 17.70

 

Synonym: 

 

ERB041

WAY-202041

 

Chemical Name:

2-(3-fluoro-4-hydroxyphenyl)-7-vinylbenzo[d]oxazol-5-ol

 

InChi Key:

MQIMZDXIAHJKQP-UHFFFAOYSA-N

 

InChi Code: 

InChI=1S/C15H10FNO3/c1-2-8-5-10(18)7-12-14(8)20-15(17-12)9-3-4-13(19)11(16)6-9/h2-7,18-19H,1H2

 

Smiles Code:

OC1=CC(C=C)=C(OC(C2=CC=C(O)C(F)=C2)=N3)C3=C1

 

 

Technical Data:

 

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: 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 Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

 

In Vitro:

Prinaberel (ERB-041) (0-60 µM; 24 hours) treatment of human SCC cells induces cell differentiation, cell cycle arrest and reduces colony formation.

Prinaberel shows a marked reduction in the expression of inflammation regulatory proteins such as p-NFκBp65, iNOS and COX-2 in A431 cells. Prinaberel diminishes phosphorylated-PI3K and -AKT, which is associated with the enhancement in E-cadherin expression and reduction in migration of A431 cells.

Prinaberel (0.01-10 µM) inhibits cell proliferation in a dose- and time-dependent manner.

Prinaberel (10 µM; 48 hours) promotes ovarian cancer (SKOV-3 cells) apoptosis.

 

In Vivo:

Prinaberel (2mg/mouse; topically; 30 min prior to UVB irradiation for 30 weeks) suppresses development of squamous cell carcinoma in SKH-1 hairless mice.

Prinaberel reduces proliferation and angiogenesis and induces apoptosis in UVB-induced skin tumors. Prinaberel suppresses pro-inflammatory signaling pathway in UVB-induced skin tumors. Prinaberel diminished tumor invasiveness via PI3K-AKT pathway and WNT signaling.

 

 

References:

 

  1. Hinsche O, Girgert R, Emons G, Gründker C. Estrogen receptor β selective agonists reduce invasiveness of triple-negative breast cancer cells. Int J Oncol. 2015 Feb;46(2):878-84. doi: 10.3892/ijo.2014.2778. Epub 2014 Nov 25. PubMed PMID: 25420519.

 

  1. Evers NM, van den Berg JH, Wang S, Melchers D, Houtman R, de Haan LH, Ederveen AG, Groten JP, Rietjens IM. Cell proliferation and modulation of interaction of estrogen receptors with coregulators induced by ERα and ERβ agonists. J Steroid Biochem Mol Biol. 2014 Sep;143:376-85. doi: 10.1016/j.jsbmb.2014.06.002. Epub 2014 Jun 9. PubMed PMID: 24923734.

 

  1. Yao PL, Gonzalez FJ, Peters JM. Targeting estrogen receptor-β for the prevention of nonmelanoma skin cancer. Cancer Prev Res (Phila). 2014 Feb;7(2):182-5. doi: 10.1158/1940-6207.CAPR-13-0409. Epub 2014 Jan 24. PubMed PMID: 24464730; PubMed Central PMCID: PMC4114311.

 

  1. Chaudhary SC, Singh T, Talwelkar SS, Srivastava RK, Arumugam A, Weng Z, Elmets CA, Afaq F, Kopelovich L, Athar M. Erb-041, an estrogen receptor-β agonist, inhibits skin photocarcinogenesis in SKH-1 hairless mice by downregulating the WNT signaling pathway. Cancer Prev Res (Phila). 2014 Feb;7(2):186-98. doi: 10.1158/1940-6207.CAPR-13-0276. Epub 2013 Nov 11. PubMed PMID: 24217507; PubMed Central PMCID: PMC3946228.

 

  1. Lattrich C, Schüler S, Häring J, Skrzypczak M, Ortmann O, Treeck O. Effects of a combined treatment with tamoxifen and estrogen receptor β agonists on human breast cancer cell lines. Arch Gynecol Obstet. 2014 Jan;289(1):163-71. doi: 10.1007/s00404-013-2977-7. Epub 2013 Aug 2. PubMed PMID: 23907354.

 

Products are for research use only. Not for human use.

 

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