Eprenetapopt (APR-246)

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WARNING: This product is for research use only, not for human or veterinary use.

Description:APR-246, also known as PRIMA-1MET and Eprenetapopt, is a quinuclidinone derivative that targets the Wrap53 gene with potential antineoplastic activity. p53 activator APR-246 binds to and activates transcription of the Wrap53 gene, which results in an increase in WRAP53 p53 antisense transcript levels and, potentially, an increase in native p53 activity; in turn, increased p53 activity may lead to an induction of cell cycle arrest and apoptosis in tumor cells. This agent may work synergistically with other antineoplastic agents.

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Eprenetapopt (APR-246), purity > 98%, is in stock. The same day shipping out after order is received.

Synonym:APR246; APR-246; APR 246. PRIMA-1MET; Eprenetapopt;

IUPAC/Chemical Name:2-(hydroxymethyl)-2-(methoxymethyl)quinuclidin-3-one

InChi Key:BGBNULCRKBVAKL-UHFFFAOYSA-N

InChi Code:InChI=1S/C10H17NO3/c1-14-7-10(6-12)9(13)8-2-4-11(10)5-3-8/h8,12H,2-7H2,1H3

SMILES Code:O=C1C(COC)(CO)N2CCC1CC2

Technical Data

Additional Information

References

1: Shalom-Feuerstein R, Serror L, Aberdam E, MüllerFJ, van Bokhoven H, Wiman KG, Zhou H, Aberdam D, Petit I. Impairedepithelial differentiation of induced pluripotent stem cells fromectodermal dysplasia-related patients is rescued by the small compoundAPR-246/PRIMA-1MET. Proc Natl Acad Sci U S A. 2013 Feb 5;110(6):2152-6.doi: 10.1073/pnas.1201753109. Epub 2013 Jan 25. PubMed PMID: 23355677.

2: Shen J, van den Bogaard EH, Kouwenhoven EN, Bykov VJ, Rinne T, ZhangQ, Tjabringa GS, Gilissen C, van Heeringen SJ, Schalkwijk J, vanBokhoven H, Wiman KG, Zhou H. APR-246/PRIMA-1MET rescues epidermaldifferentiation in skin keratinocytes derived from EEC syndrome patientswith p63 mutations. Proc Natl Acad Sci U S A. 2013 Feb 5;110(6):2157-62.doi: 10.1073/pnas.1201993110. Epub 2013 Jan 25. PubMed PMID: 23355676.

3: Lehmann S, Bykov VJ, Ali D, Andrén O, Cherif H, Tidefelt U, Uggla B,Yachnin J, Juliusson G, Moshfegh A, Paul C, Wiman KG, Andersson PO.Targeting p53 in vivo: a first-in-human study with p53-targetingcompound APR-246 in refractory hematologic malignancies and prostatecancer. J Clin Oncol. 2012 Oct 10;30(29):3633-9. doi:10.1200/JCO.2011.40.7783. Epub 2012 Sep 10. PubMed PMID: 22965953.

4: Zandi R, Selivanova G, Christensen CL, Gerds TA, Willumsen BM,Poulsen HS. PRIMA-1Met/APR-246 induces apoptosis and tumor growth delayin small cell lung cancer expressing mutant p53. Clin Cancer Res. 2011May 1;17(9):2830-41. doi: 10.1158/1078-0432.CCR-10-3168. Epub 2011 Mar17. PubMed PMID: 21415220.

5: Bao W, Chen M, Zhao X, Kumar R, Spinnler C, Thullberg M, Issaeva N,Selivanova G, Strömblad S. PRIMA-1Met/APR-246 induces wild-typep53-dependent suppression of malignant melanoma tumor growth in 3Dculture and in vivo. Cell Cycle. 2011 Jan 15;10(2):301-7. Epub 2011 Jan15. PubMed PMID: 21239882.

6: Ali D, Jönsson-Videsäter K, Deneberg S, Bengtzén S, Nahi H, Paul C,Lehmann S. APR-246 exhibits anti-leukemic activity and synergism withconventional chemotherapeutic drugs in acute myeloid leukemia cells. EurJ Haematol. 2011 Mar;86(3):206-15. doi:10.1111/j.1600-0609.2010.01557.x. Epub 2011 Jan 11. PubMed PMID:21114538.

7: Rökaeus N, Shen J, Eckhardt I, Bykov VJ, Wiman KG, Wilhelm MT.PRIMA-1(MET)/APR-246 targets mutant forms of p53 family members p63 andp73. Oncogene. 2010 Dec 9;29(49):6442-51. doi: 10.1038/onc.2010.382.Epub 2010 Sep 6. PubMed PMID: 20818419.

我国旅美科学家陈清奇博士创立的MedKoo美帝药库医药公司目前正在建立全球第一个小分子抗癌药库。 MedKoo是一家以研发、生产和销售小分子抗癌化合物为主的医药科技公司。 业务范围 为全球所有从事抗癌药物研究和开发的制药公司，高校，研究院所，政府相关机构提供与抗癌药物分子相关的产品、试剂和技术服务。 技术核心 以药物化学合成技术为核心，密切结合全球抗癌新药研发领域中的新技术、新理论、新趋势和新的发展方向，不断推出抗癌化合物新品种。 建造目标 MedKoo美帝药库的目标是：建成全球最大的小分子抗癌药库 ，品种最多最全、质量最好最可靠。美帝药库的宗旨是：客户第一；质量第一；信誉第一；创新第一。