Delimotecan

• CAT Number: I006428
• CAS Number: 187852-63-7
• Molecular Formula: C31H36N6O8
• Molecular Weight: 620.663
• Purity: ≥95%
• Synonyms: Delimotecan; MEN-4901; MEN4901; MEN 4901; T-0128; T 0128; T0128;(S)-2-amino-N-(2-((2-((3-((4,11-diethyl-4-hydroxy-3,14-dioxo-3,4,12,14-tetrahydro-1H-pyrano[3/’,4/’:6,7]indolizino[1,2-b]quinolin-9-yl)oxy)propyl)amino)-2-oxoethyl)amino)-2-oxoethyl)acet
• Target: DNA Topoisomerase I Inhibitor
• Solubility: Soluble in DMSO
• Storage: 0 - 4°C for short term or -20 °C for long term
• InChI: InChI=1S/C31H36N6O8/c1-3-18-19-10-17(44-9-5-8-33-26(39)13-35-27(40)14-34-25(38)12-32)6-7-23(19)36-28-20(18)15-37-24(28)11-22-21(29(37)41)16-45-30(42)31(22,43)4-2/h6-7,10-11,43H,3-5,8-9,12-16,32H2,1-2H3,(H,33,39)(H,34,38)(H,35,40)/t31-/m0/s1
• InChIKey: MWOPHYKKEDTKAZ-HKBQPEDESA-N
• SMILES: CCC1=C2C=C(C=CC2=NC3=C1CN4C3=CC5=C(C4=O)COC(=O)C5(CC)O)OCCCNC(=O)CNC(=O)CNC(=O)CN

Delimotecan, also known as MEN-4901 and T-0128, is a DNA topoisomerase I inhibitor potentially for the treatment of solid tumors. Delimotecan had a long terminal half-life of 109 h, and relatively high exposures to T-2513 and SN-38 were obtained. The percentage decrease in WBC and absolute neutrophil count significantly correlated with the dose of delimotecan.

Reference

1:Antitumor activity of delimotecan against human metastatic melanoma: pharmacokinetics and molecular determinants. Bigioni M, Parlani M, Bressan A, Bellarosa D, Rivoltini L, Animati F, Crea A, Bugianesi R, Maggi CA, Manzini S, Binaschi M.Int J Cancer. 2009 Nov 15;125(10):2456-64. doi: 10.1002/ijc.24661. PMID: 19536774 Free Article2:Clinical and pharmacologic study of the novel prodrug delimotecan (MEN 4901/T-0128) in patients with solid tumors. Veltkamp SA, Witteveen EO, Capriati A, Crea A, Animati F, Voogel-Fuchs M, van den Heuvel IJ, Beijnen JH, Voest EE, Schellens JH.Clin Cancer Res. 2008 Nov 15;14(22):7535-44. doi: 10.1158/1078-0432.CCR-08-0438. PMID: 19010872 Free Article