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Rosabulin

  

Description of Rosabulin: rosabulin (STA-5312) is a novel microtubule inhibitor with a distinct binding site from other agents such as vincristine, colchicine, or paclitaxel, which has demonstrated antitumor activity against a range of solid tumors in chemotherapy-resistant cancer. Phase I study showed that STA-5312 appears to be well tolerated when given weekly in doses up to 32mg/m2. The MTD has not been determined and enrollment is ongoing. (source: asco.org)

  

Current developer:  Synta Pharmaceuticals Corp.

  

MedKoo Cat#: 202510

Name: Rosabulin

CAS#: 501948-05-6

 

Synonym: STA-5312;

  

IUPAC/Chemical name: 

3-[(4-Cyanophenyl)methyl]-N-(3-methyl-5-isothiazolyl)-alpha-oxo-1-indolizineacetamide

 

Chemical structure: Theoretical analysis :

 

  

Chemical Formula: C22H16N4O2S

Exact Mass: 400.09940

Molecular Weight: 400.45

Elemental Analysis: C, 65.98; H, 4.03; N, 13.99; O, 7.99; S, 8.01

   

 

 

  

Availability and price:

  

 Rosabulin is available through custom synthesis.

To inquire the quotation and lead time of custom synthesis for this agent, please send email to sales@medkoo.com to describe your needs. A representative will respond your email shortly. We offer big discount for orders of bulk quantities.

 

Quality control data:

Product will be shipped with supporting analytical data.

 

 

Information about this agent

STA-5312, 2-[3-(4-cyano-benzyl)-indolizin-1-yl]-N-(3-methyl-isothiazol-5-yl)-2-oxo-acetamide, is a new chemical entity being developed for the treatment of chemotherapy-resistant tumors. STA-5312 demonstrates substantial anti-proliferative activity against a wide range of cancer cell linesin vitro, with IC50 values extending down into the nanomolar range. The in vitro cytotoxic effects have been demonstrated across a wide array of tumor types, including hematologic and solid tumor cell lines of various origins (e.g. leukemia, lymphoma, breast, colon, uterine). Cell lines with multi-drug resistant (MDR) phenotypes were similarly sensitive to STA-5312. The mechanism of action for STA-5312 is inhibition of microtubule assembly and subsequent arrest of the cell cycle. STA-5312 is active against several tumor cell lines that express moderate to high levels of P-glycoprotein (Pgp), including lines insensitive to Taxol, Vincristine, and Adriamycin in which Pgp activity is a major contributor to the MDR phenotype. When dosed orally or intravenously, STA-5312 has shown in vivo activity in several murine tumors as well as human tumor xenograft models, including drug resistant tumors. Data on the murine leukemia P388 suggested activity in a vincristine-resistant cell line, and data in the RL human Lymphoma cell line suggested an additive effect of Taxol plus STA-5312. Thus, STA-5312 is a potential new therapy for the treatment of cancer including chemoresistant tumors. Considering the breadth of antitumor activity demonstrated by STA-5312 both in vitro and in vivo, two lines of clinical investigation are envisioned encompassing both hematologic and solid tumors. see: Synta Pharmaceuticals Corp's meeting abstract.

 

STA-5312 inhibits microtubule function, critical to cancer cell proliferation, through a unique binding site. Ongoing phase 1 studies of STA- 5312 in hematological and solid tumor malignancies are expected to be completed in the first half of 2006. The study findings will guide future clinical investment decisions for the compound.

  

 

References:

 1: Chen G, Wang ZQ, Jia JM. Three minor novel triterpenoids from the leaves of Diospyros kaki. Chem Pharm Bull (Tokyo). 2009 May;57(5):532-5. PubMed PMID: 19420791.

2: Park JC, Kim SC, Choi MR, Song SH, Yoo EJ, Kim SH, Miyashiro H, Hattori M. Anti-HIV protease activity from rosa family plant extracts and rosamultin from Rosa rugosa. J Med Food. 2005 Spring;8(1):107-9. PubMed PMID: 15857219.

3: Cheol Park J, Chul Kim S, Moon Hur J, Choi SH, Yeon Lee K, Won Choi J. Anti-hepatotoxic effects of Rosa rugosa root and its compound, rosamultin, in rats intoxicated with bromobenzene. J Med Food. 2004 Winter;7(4):436-41. PubMed PMID: 15671686.

4: Jung HJ, Nam JH, Choi J, Lee KT, Park HJ. 19Alpha-hydroxyursane-type triterpenoids: antinociceptive anti-inflammatory principles of the roots of Rosa rugosa. Biol Pharm Bull. 2005 Jan;28(1):101-4. PubMed PMID: 15635171.

5: Cho EJ, Yokozawa T, Rhyu DY, Kim HY, Shibahara N, Park JC. The inhibitory effects of 12 medicinal plants and their component compounds on lipid peroxidation. Am J Chin Med. 2003;31(6):907-17. PubMed PMID: 14992543.

6: Lu X, Xu W, Shen J, Han G. [Chemical studies on Campylotropis hirtella (Franch. Schindl.)]. Zhongguo Zhong Yao Za Zhi. 1997 Nov;22(11):680-2, 704. Chinese. PubMed PMID: 11243186.

7: Rücker G, Mayer R, Shin-Kim JS. [Triterpene saponins from the Chinese drug "Daxueteng" (Caulis sargentodoxae)]. Planta Med. 1991 Oct;57(5):468-70. German. PubMed PMID: 1798803.

8: Wang XY. [Effects of constituents of the roots of Rosa multiflora on hyperlipemia]. Zhong Yao Tong Bao. 1986 Jun;11(6):55-6. Chinese. PubMed PMID: 2948697.

 

 

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