A DNA topoisomerase I inhibitor
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Belotecan (hydrochloride)

Item No. 35488

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(4S)-4-ethyl-4-hydroxy-11-[2-[(1-methylethyl)amino]ethyl]-1H-pyrano[3′,4′:6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione, monohydrochloride
CAS Number
213819-48-8
Synonyms
  • 7-[2-(N-isopropylamino)ethyl]-(20S)-Camptothecin
  • CKD602
  • (S)-CKD602
Molecular Formula
C25H27N3O4 • HCl
Formula Weight
470.0
Purity
≥95%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 14 mg/mlEthanol: Slightly solublePBS (pH 7.2): 0.16 mg/ml
λmax
220, 254, 362 nm
SMILES
O=C1N2C(C3=NC4=CC=CC=C4C(CCNC(C)C)=C3C2)=CC5=C1COC([C@]5(O)CC)=O.Cl
InChi Code
InChI=1S/C25H27N3O4.ClH/c1-4-25(31)19-11-21-22-17(12-28(21)23(29)18(19)13-32-24(25)30)15(9-10-26-14(2)3)16-7-5-6-8-20(16)27-22;/h5-8,11,14,26,31H,4,9-10,12-13H2,1-3H3;1H/t25-;/m0./s1
InChi Key
SJKBXKKZBKCHET-UQIIZPHYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $69

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    10 mg

    $130

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    50 mg

    $291

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    100 mg

    $410

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    Cayman Chemical
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    Product Description

    Belotecan is an inhibitor of DNA topoisomerase I (IC50 = 0.119 µg/ml) and a derivative of the DNA topoisomerase I inhibitor camptothecin (Item No. 11694).1 It inhibits the proliferation of various cancer cell lines, including KATO III stomach, HT-29 colon, A549 lung, MDA-MB-231 breast, and SKOV3 ovarian cancer cells (IC50s = 160, 10.9, 9, 345, and 31 ng/ml, respectively). Belotecan (150 ng/ml) induces apoptosis and cell cycle arrest at the G2/M phase in, and inhibits invasion of, SiHa cervical cancer cells.2 It reduces tumor growth in a Ca Ski cervical cancer mouse xenograft model when administered at a dose of 25 mg/kg. Belotecan (80 µg/kg) reduces food intake and body weight in pregnant dams and increases fetal deaths and decreases litter size.3 Formulations containing belotecan have been used in the treatment of ovarian and small cell lung cancer.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Lee, J.H., Lee, J.M., Kim, J.K., et al. Antitumor activity of 7-[2-(N-isopropylamino)ethyl]-(20S)-camptothecin, CKD602, as a potent DNA topoisomerase I inhibitor. Arch. Pharm. Res. 21(5), 581-590 (1998).

    2. Lee, S., Ho, J.Y., Liu, J.J., et al. CKD-602, a topoisomerase I inhibitor, induces apoptosis and cell-cycle arrest and inhibits invasion in cervical cancer. Mol. Med. 25(1), 23 (2019).

    3. Chung, M.-K., Kim, J.-C., and Han, S.-S. Embryotoxic effects of CKD-602, a new camptothecin anticancer agent, in rats. Reprod. Toxicol. 20(1), 165-173 (2005).