A DNA topoisomerase I inhibitor
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Exatecan (mesylate)

Item No. 35452

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(1S,9S)-1-amino-9-ethyl-5-fluoro-1,2,3,9,12,15-hexahydro-9-hydroxy-4-methyl-10H,13H-benzo[de]pyrano[3′,4′:6,7]indolizino[1,2-b]quinoline-10,13-dione, monomethanesulfonate
CAS Number
169869-90-3
Synonyms
  • DX 8951f
Molecular Formula
C24H22FN3O4 • CH3SO3H
Formula Weight
531.6
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: soluble
λmax
224, 261, 337 nm
SMILES
CS(=O)(O)=O.N[C@@H]1C2=C3C(C(N4C3)=CC([C@](O)(C(OC5)=O)CC)=C5C4=O)=NC6=CC(F)=C(C)C(CC1)=C62
InChi Code
InChI=1S/C24H22FN3O4.CH4O3S/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;1-5(2,3)4/h6-7,16,31H,3-5,8-9,26H2,1-2H3;1H3,(H,2,3,4)/t16-,24-;/m0./s1
InChi Key
BICYDYDJHSBMFS-GRGFAMGGSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

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    25 mg

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    50 mg

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    Cayman Chemical
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    Product Description

    Exatecan is a derivative of camptothecin (Item No. 11694) and DNA topoisomerase I inhibitor (IC50 = 0.975 µg/ml).1 It inhibits cell growth in a panel of 32 breast, colon, stomach, and lung cancer cell lines (GI50s = 0.125-10.4 ng/ml). Exatecan (3.325-50 mg/kg) reduces tumor growth in an SC-6-JCK gastric adenocarcinoma mouse xenograft model. It reduces tumor weight in HCT116, PC-6, and PC12 mouse xenograft models when administered at a dose of 75 mg/kg.2 Exatecan has also been used in the synthesis of cytotoxic payload moieties of antibody-drug conjugates (ADCs).3 Formulations containing exatecan have been used in the treatment of breast, gastric, and gastroesophageal cancers.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Mitsui, I., Kumazawa, E., Hirota, Y., et al. A new water-soluble camptothecin derivative, DX-8951f, exhibits potent antitumor activity against human tumors in vitro and in vivo. Jpn. J. Cancer Res. 86(8), 776-782 (1995).

    2. Kumazawa, E., and Ochi, Y. DE-310, a novel macromolecular carrier system for the camptothecin analog DX-8951f: Potent antitumor activities in various murine tumor models. Cancer Sci. 95(2), 168-175 (2004).

    3. Conilh, L., Fournet, G., Fourmaux, E., et al. Exatecan antibody drug conjugates based on a hydrophilic polysarcosine drug-linker platform. Pharmaceuticals (Basel) 14(3), 247 (2021).