Belinostat
Belinostat is a novel hydroxamic acid-type histone deacetylase (HDAC) inhibitor with antineoplastic activity. Belinostat targets HDAC enzymes, thereby inhibiting tumor cell proliferation, inducing apoptosis, promoting cellular differentiation, and inhibiting angiogenesis. This agent may sensitize drug-resistant tumor cells to other antineoplastic agents, possibly through a mechanism involving the down-regulation of thymidylate synthase. Belinostat was approved in 2014 for relapsed or refractory peripheral T-cell lymphoma.
1: Odenike O, Halpern A, Godley LA, Madzo J, Karrison T, Green M, Fulton N, Mattison RJ, Yee KW, Bennett M, Koval G, Malnassy G, Larson RA, Ratain MJ, Stock W. A phase I and pharmacodynamic study of the histone deacetylase inhibitor belinostat plus azacitidine in advanced myeloid neoplasia. Invest New Drugs. 2014 Dec 9. [Epub ahead of print] PubMed PMID: 25483416.
2: Kim MJ, Lee JS, Park SE, Yi HJ, Jeong IG, Kang JS, Yun J, Lee JY, Ro S, Lee JS, Choi EK, Hwang JJ, Kim CS. Combination treatment of renal cell carcinoma with belinostat and 5-fluorouracil: A role for oxidative stress-induced DNA damage and HSP90-regulated thymidine synthase. J Urol. 2014 Nov 26. pii: S0022-5347(14)05012-5. doi: 10.1016/j.juro.2014.11.091. [Epub ahead of print] PubMed PMID: 25433307.
3: Foss F, Advani R, Duvic M, Hymes KB, Intragumtornchai T, Lekhakula A, Shpilberg O, Lerner A, Belt RJ, Jacobsen ED, Laurent G, Ben-Yehuda D, Beylot-Barry M, Hillen U, Knoblauch P, Bhat G, Chawla S, Allen LF, Pohlman B. A Phase II trial of Belinostat (PXD101) in patients with relapsed or refractory peripheral or cutaneous T-cell lymphoma. Br J Haematol. 2014 Nov 17. doi: 10.1111/bjh.13222. [Epub ahead of print] PubMed PMID: 25404094.
4: Bodiford A, Bodge M, Talbott MS, Reddy NM. Profile of belinostat for the treatment of relapsed or refractory peripheral T-cell lymphoma. Onco Targets Ther. 2014 Oct 24;7:1971-7. doi: 10.2147/OTT.S59269. eCollection 2014. Review. PubMed PMID: 25368524; PubMed Central PMCID: PMC4216035.
5: Thomas A, Rajan A, Szabo E, Tomita Y, Carter CA, Scepura B, Lopez-Chavez A, Lee MJ, Redon CE, Frosch A, Peer CJ, Chen Y, Piekarz R, Steinberg SM, Trepel JB, Figg WD, Schrump DS, Giaccone G. A phase I/II trial of belinostat in combination with cisplatin, doxorubicin, and cyclophosphamide in thymic epithelial tumors: a clinical and translational study. Clin Cancer Res. 2014 Nov 1;20(21):5392-402. doi: 10.1158/1078-0432.CCR-14-0968. Epub 2014 Sep 4. PubMed PMID: 25189481; PubMed Central PMCID: PMC4216756.
6: Poole RM. Belinostat: first global approval. Drugs. 2014 Sep;74(13):1543-54. doi: 10.1007/s40265-014-0275-8. PubMed PMID: 25134672.
7: Thompson CA. Belinostat approved for use in treating rare lymphoma. Am J Health Syst Pharm. 2014 Aug 15;71(16):1328. doi: 10.2146/news140056. PubMed PMID: 25074945.
8: McDermott J, Jimeno A. Belinostat for the treatment of peripheral T-cell lymphomas. Drugs Today (Barc). 2014 May;50(5):337-45. doi: 10.1358/dot.2014.50.5.2138703. Review. PubMed PMID: 24918834.
9: Savickiene J, Treigyte G, Valiuliene G, Stirblyte I, Navakauskiene R. Epigenetic and molecular mechanisms underlying the antileukemic activity of the histone deacetylase inhibitor belinostat in human acute promyelocytic leukemia cells. Anticancer Drugs. 2014 Sep;25(8):938-49. doi: 10.1097/CAD.0000000000000122. PubMed PMID: 24800886.
10: Kirschbaum MH, Foon KA, Frankel P, Ruel C, Pulone B, Tuscano JM, Newman EM. A phase 2 study of belinostat (PXD101) in patients with relapsed or refractory acute myeloid leukemia or patients over the age of 60 with newly diagnosed acute myeloid leukemia: a California Cancer Consortium Study. Leuk Lymphoma. 2014 Oct;55(10):2301-4. doi: 10.3109/10428194.2013.877134. Epub 2014 Feb 24. PubMed PMID: 24369094; PubMed Central PMCID: PMC4143479.
2: Kim MJ, Lee JS, Park SE, Yi HJ, Jeong IG, Kang JS, Yun J, Lee JY, Ro S, Lee JS, Choi EK, Hwang JJ, Kim CS. Combination treatment of renal cell carcinoma with belinostat and 5-fluorouracil: A role for oxidative stress-induced DNA damage and HSP90-regulated thymidine synthase. J Urol. 2014 Nov 26. pii: S0022-5347(14)05012-5. doi: 10.1016/j.juro.2014.11.091. [Epub ahead of print] PubMed PMID: 25433307.
3: Foss F, Advani R, Duvic M, Hymes KB, Intragumtornchai T, Lekhakula A, Shpilberg O, Lerner A, Belt RJ, Jacobsen ED, Laurent G, Ben-Yehuda D, Beylot-Barry M, Hillen U, Knoblauch P, Bhat G, Chawla S, Allen LF, Pohlman B. A Phase II trial of Belinostat (PXD101) in patients with relapsed or refractory peripheral or cutaneous T-cell lymphoma. Br J Haematol. 2014 Nov 17. doi: 10.1111/bjh.13222. [Epub ahead of print] PubMed PMID: 25404094.
4: Bodiford A, Bodge M, Talbott MS, Reddy NM. Profile of belinostat for the treatment of relapsed or refractory peripheral T-cell lymphoma. Onco Targets Ther. 2014 Oct 24;7:1971-7. doi: 10.2147/OTT.S59269. eCollection 2014. Review. PubMed PMID: 25368524; PubMed Central PMCID: PMC4216035.
5: Thomas A, Rajan A, Szabo E, Tomita Y, Carter CA, Scepura B, Lopez-Chavez A, Lee MJ, Redon CE, Frosch A, Peer CJ, Chen Y, Piekarz R, Steinberg SM, Trepel JB, Figg WD, Schrump DS, Giaccone G. A phase I/II trial of belinostat in combination with cisplatin, doxorubicin, and cyclophosphamide in thymic epithelial tumors: a clinical and translational study. Clin Cancer Res. 2014 Nov 1;20(21):5392-402. doi: 10.1158/1078-0432.CCR-14-0968. Epub 2014 Sep 4. PubMed PMID: 25189481; PubMed Central PMCID: PMC4216756.
6: Poole RM. Belinostat: first global approval. Drugs. 2014 Sep;74(13):1543-54. doi: 10.1007/s40265-014-0275-8. PubMed PMID: 25134672.
7: Thompson CA. Belinostat approved for use in treating rare lymphoma. Am J Health Syst Pharm. 2014 Aug 15;71(16):1328. doi: 10.2146/news140056. PubMed PMID: 25074945.
8: McDermott J, Jimeno A. Belinostat for the treatment of peripheral T-cell lymphomas. Drugs Today (Barc). 2014 May;50(5):337-45. doi: 10.1358/dot.2014.50.5.2138703. Review. PubMed PMID: 24918834.
9: Savickiene J, Treigyte G, Valiuliene G, Stirblyte I, Navakauskiene R. Epigenetic and molecular mechanisms underlying the antileukemic activity of the histone deacetylase inhibitor belinostat in human acute promyelocytic leukemia cells. Anticancer Drugs. 2014 Sep;25(8):938-49. doi: 10.1097/CAD.0000000000000122. PubMed PMID: 24800886.
10: Kirschbaum MH, Foon KA, Frankel P, Ruel C, Pulone B, Tuscano JM, Newman EM. A phase 2 study of belinostat (PXD101) in patients with relapsed or refractory acute myeloid leukemia or patients over the age of 60 with newly diagnosed acute myeloid leukemia: a California Cancer Consortium Study. Leuk Lymphoma. 2014 Oct;55(10):2301-4. doi: 10.3109/10428194.2013.877134. Epub 2014 Feb 24. PubMed PMID: 24369094; PubMed Central PMCID: PMC4143479.
| Chemical | |
|---|---|
| CAS Num | 414864-00-9 |
| Chemical Formula | C15H14N2O4S |
| Molecular Weight | 318.34 |
| IUPAC Chemical Name | (E)-N-hydroxy-3-[3-(phenylsulfamoyl)phenyl]prop-2-enamide. |
| Exact Mass | 318.06743 |
| Elemental Analysis | C, 56.59; H, 4.43; N, 8.80; O, 20.10; S, 10.07. |
| Synonym | PXD 101; PXD101; PXD-101; PX105684; PX-105684; PX 105684; NSC726630; brand name |
| Solubility | Soluble in DMSO, not in water |
| SMILES Code | O=C(NO)/C=C/C1=CC=CC(S(=O)(NC2=CC=CC=C2)=O)=C1 |
| Biological | |
| Targets and Effects | istone deacetylases (HDAC) inhibitor |
| Pathways | Apoptosis |
| Physical | |
| Appearance | White 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). |
| Shelf Life | >2 years if stored properly |
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