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MedKoo product information:

 

  Bizelesin  

     

Description of Bizelesin:  Bizelesin is a synthetic cyclopropylpyrroloindole antineoplastic antibiotic. Bizelesin binds to the minor groove of DNA and induces interstrand cross-linking of DNA, thereby inhibiting DNA replication and RNA synthesis. Bizelesin also enhances p53 and p21 induction and triggers G2/M cell-cycle arrest, resulting in cell senescence without apoptosis. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

 

Current developer:

 

MedKoo Cat#: 205951

Name:  Bizelesin

CAS#:  129655-21-6

  

Synonym: U-77779.

  

IUPAC/Chemical name: 

1,3-bis(2-((S)-1-(chloromethyl)-5-hydroxy-8-methyl-1,2,3,6-tetrahydropyrrolo[3,2-e]indole-3-carbonyl)-1H-indol-5-yl)urea  

  

Chemical structure

Theoretical analysis

 

Bizelesin chemical structure

 

 

Chemical Formula: C43H36Cl2N8O5
Exact Mass: 814.21857
Molecular Weight: 815.70
Elemental Analysis: C, 63.31; H, 4.45; Cl, 8.69; N, 13.74; O, 9.81

 

  

Availability and price:

 

This agent is not in stock, which may be available through  custom synthesis.

  

 

To inquire quotation and lead time or to ask questions, 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.

 

 

Highlights of recent research using this agent

  

 

 

References

1: Cao PR, McHugh MM, Melendy T, Beerman T. The DNA minor groove-alkylating cyclopropylpyrroloindole drugs adozelesin and bizelesin induce different DNA damage response pathways in human colon carcinoma HCT116 cells. Mol Cancer Ther. 2003 Jul;2(7):651-9. PubMed PMID: 12883038.

2: Schwartz GH, Patnaik A, Hammond LA, Rizzo J, Berg K, Von Hoff DD, Rowinsky EK. A phase I study of bizelesin, a highly potent and selective DNA-interactive agent, in patients with advanced solid malignancies. Ann Oncol. 2003 May;14(5):775-82. PubMed PMID: 12702533.

3: Pitot HC, Reid JM, Sloan JA, Ames MM, Adjei AA, Rubin J, Bagniewski PG, Atherton P, Rayson D, Goldberg RM, Erlichman C. A Phase I study of bizelesin (NSC 615291) in patients with advanced solid tumors. Clin Cancer Res. 2002 Mar;8(3):712-7. PubMed PMID: 11895900.

4: McHugh MM, Kuo SR, Walsh-O'Beirne MH, Liu JS, Melendy T, Beerman TA. Bizelesin, a bifunctional cyclopropylpyrroloindole alkylating agent, inhibits simian virus 40 replication in trans by induction of an inhibitor. Biochemistry. 1999 Aug 31;38(35):11508-15. PubMed PMID: 10471303.

5: Hidalgo M, Izbicka E, Cerna C, Gomez L, Rowinsky EK, Weitman SD, Von Hoff DD. Comparative activity of the cyclopropylpyrroloindole compounds adozelesin, bizelesin and carzelesin in a human tumor colony-forming assay. Anticancer Drugs. 1999 Mar;10(3):295-302. PubMed PMID: 10327036.

6: Woynarowski JM, Chapman WG, Napier C, Herzig MC. Induction of AT-specific DNA-interstrand crosslinks by bizelesin in genomic and simian virus 40 DNA. Biochim Biophys Acta. 1999 Feb 16;1444(2):201-17. PubMed PMID: 10023060.

7: Woynarowski JM, Beerman TA. Effects of bizelesin (U-77,779), a bifunctional alkylating minor groove binder, on replication of genomic and simian virus 40 DNA in BSC-1 cells. Biochim Biophys Acta. 1997 Jul 17;1353(1):50-60. PubMed PMID: 9256064.

8: Carter CA, Waud WR, Li LH, DeKoning TF, McGovren JP, Plowman J. Preclinical antitumor activity of bizelesin in mice. Clin Cancer Res. 1996 Jul;2(7):1143-9. PubMed PMID: 9816280.

9: Volpe DA, Tomaszewski JE, Parchment RE, Garg A, Flora KP, Murphy MJ, Grieshaber CK. Myelotoxic effects of the bifunctional alkylating agent bizelesin on human, canine and murine myeloid progenitor cells. Cancer Chemother Pharmacol. 1996;39(1-2):143-9. PubMed PMID: 8995512.

10: Woynarowski JM, McHugh MM, Gawron LS, Beerman TA. Effects of bizelesin (U-77779), a bifunctional alkylating minor groove agent, on genomic and simian virus 40 DNA. Biochemistry. 1995 Oct 10;34(40):13042-50. PubMed PMID: 7548063.

   

 

 

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