Camptothecin

- Overview
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    Background
    
    Camptothecin is a selective inhibitor of topoisomerase I with IC50 value of 679 nM [1].
    Camptothecin could induce cell death in SMMC-7721, MCF-7, and HCT-116 tumor cells. Camptothecin has been reported to induce autophagy via AMPK-TSC2-mTOR pathway, at the mean time, induce premature senescence by ATM-Chk2-p53-p21 pathway [2].
    Studies indicated that camptothecin had anti-tumor activity in (non-small cell lung cancer) NSCLC xenografts. Camptothecin -induced DNA damage has revealed to cause phosphorylation of H2AX (γH2AX). Previous studies have also demonstrated to reduce the expression of Top1 in cancer cells treated with camptothecins [3].
    
    [1] Luzzio MJ1, Besterman JM, Emerson DL, Evans MG, Lackey K, Leitner PL, McIntyre G, Morton B, Myers PL, Peel M, et al. Synthesis and antitumor activity of novel water soluble derivatives of camptothecin as specific inhibitors of topoisomerase I. J Med Chem. 1995 Feb 3;38(3):395-401.
    [2] Zhang JW1, Zhang SS1, Song JR2, Sun K3, Zong C1, Zhao QD1, Liu WT1, Li R1, Wu MC1, Wei LX4. Autophagy inhibition switches low-dose camptothecin-induced premature senescence to apoptosis in human colorectal cancer cells. Biochem Pharmacol. 2014 May 22. pii: S0006-2952(14)00286-X.
    [3] Tsakalozou E1, Adane ED, Liang Y, Arnold SM, Leggas M. Protracted dosing of the lipophilic camptothecin analogue AR-67 in non-small cell lung cancer xenografts and humans. Cancer Chemother Pharmacol. 2014 May 8. [Epub ahead of print]
- Properties
  - Alternative Name
    
    (S)-4-ethyl-4-hydroxy-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione
    
    CAS Number
    
    7689-03-4
    
    Molecular Formula
    
    C20H16N2O4
    
    Molecular Weight
    
    348.35
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in H2O; insoluble in EtOH; ≥8.7 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Nanda Kumar Sasi, Flavie Coquel, et al. "DDK has a primary role in processing stalled replication forks to initiate downstream checkpoint signaling." bioRxiv. 2017.October 21.

Camptothecin

Background

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