Exatecan

  • CAT Number: I002235
  • CAS Number: 171335-80-1
  • Molecular Formula: C24H22FN3O4
  • Molecular Weight: 435.45
  • Purity: ≥95%
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Exatecan (CAT: I002235), also known as DX-8951f or SN-38b, is a synthetic topoisomerase I inhibitor. It is derived from the active metabolite of irinotecan, SN-38. Exatecan inhibits the action of the topoisomerase I enzyme, preventing the resealing of DNA strands during replication and transcription processes. This leads to the accumulation of DNA strand breaks and ultimately causes cell death. Exatecan has demonstrated potent anticancer activity, particularly against a variety of solid tumors. It has shown efficacy in clinical trials for the treatment of ovarian, lung, colorectal, and breast cancers. Exatecan represents a valuable option in cancer therapy, offering a targeted approach to inhibit tumor cell growth and proliferation.

Catalog Number I002235
CAS Number 171335-80-1
Molecular Formula

C24H22FN3O4

Purity 95%
Target topoisomerase I
Solubility 10 mM in DMSO
Storage 3 years -20C powder
Overview of Clinical Research

<span style=”color:#000000;”><span style=”font-size:12px;”><span style=”font-family:arial,helvetica,sans-serif;”>Exatecan is a&nbsp;DNA topoisomerase I inhibitor developed by&nbsp;Daiichi Sankyo Company. It has been granted for the new molecular entity.&nbsp;</span></span></span>

IUPAC Name (10S,23S)-23-amino-10-ethyl-18-fluoro-10-hydroxy-19-methyl-8-oxa-4,15-diazahexacyclo[14.7.1.02,14.04,13.06,11.020,24]tetracosa-1,6(11),12,14,16,18,20(24)-heptaene-5,9-dione
InChI InChI=1S/C24H22FN3O4/c1-3-24(31)14-6-18-21-12(8-28(18)22(29)13(14)9-32-23(24)30)19-16(26)5-4-11-10(2)15(25)7-17(27-21)20(11)19/h6-7,16,31H,3-5,8-9,26H2,1-2H3/t16-,24-/m0/s1
InChIKey ZVYVPGLRVWUPMP-FYSMJZIKSA-N
SMILES O=C1[C@](O)(CC)C2=C(CO1)C(N3CC4=C5C6=C(CC[C@@H]5N)C(C)=C(F)C=C6N=C4C3=C2)=O
Reference

1:Pharmacokinetics and pharmacodynamics of orally administered ruxolitinib (INCB018424 phosphate) in renal and hepatic impairment patients. Chen X, Shi JG, Emm T, Scherle PA, McGee RF, Lo Y, Landman RR, Punwani NG, Williams WV, Yeleswaram S.Clin Pharmacol Drug Dev. 2014 Jan;3(1):34-42. doi: 10.1002/cpdd.77. Epub 2013 Oct 19. PMID: 27128228<br />
2:Population pharmacokinetic analysis of orally-administered ruxolitinib (INCB018424 Phosphate) in patients with primary myelofibrosis (PMF), post-polycythemia vera myelofibrosis (PPV-MF) or post-essential thrombocythemia myelofibrosis (PET MF). Chen X, Williams WV, Sandor V, Yeleswaram S.J Clin Pharmacol. 2013 Jul;53(7):721-30. doi: 10.1002/jcph.102. Epub 2013 May 16. PMID: 23677817<br />
3:The effect of CYP3A4 inhibition or induction on the pharmacokinetics and pharmacodynamics of orally administered ruxolitinib (INCB018424 phosphate) in healthy volunteers. Shi JG, Chen X, Emm T, Scherle PA, McGee RF, Lo Y, Landman RR, McKeever EG Jr, Punwani NG, Williams WV, Yeleswaram S.J Clin Pharmacol. 2012 Jun;52(6):809-18. doi: 10.1177/0091270011405663. Epub 2011 May 20. PMID: 21602517<br />
4:The pharmacokinetics, pharmacodynamics, and safety of orally dosed INCB018424 phosphate in healthy volunteers. Shi JG, Chen X, McGee RF, Landman RR, Emm T, Lo Y, Scherle PA, Punwani NG, Williams WV, Yeleswaram S.J Clin Pharmacol. 2011 Dec;51(12):1644-54. doi: 10.1177/0091270010389469. Epub 2011 Jan 21. PMID: 21257798

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