喜树碱是拓扑异构酶I的选择性抑制剂，IC50值为679 nM [1]。

喜树碱可以诱导SMMC-7721、MCF-7和HCT-116肿瘤细胞的死亡。据报道，喜树碱通过AMPK-TSC2-mTOR途径诱导自噬，同时通过ATM-Chk2-p53-p21途径诱导早衰[2]。 研究表明喜树碱在非小细胞肺癌异种移植物中具有抗肿瘤活性。已经发现喜树碱诱导的DNA损伤导致H2AX (γH2AX)的磷酸化。以前的研究也证明了在用喜树碱治疗的癌细胞中减少Top1的表达[3]。

产品性质：

Cas No.:7689-03-4

别名:喜树碱; Campathecin; (S)-(+)-Camptothecin; CPT

化学名:(S)-4-ethyl-4-hydroxy-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione

Canonical SMILES:O=C(N(CC1=CC(C=CC=C2)=C2N=C13)C3=C4)C(CO5)=C4[C@@](O)(CC)C5=O

分子式:C20H16N2O4

分子量:348.35

溶解度:≥ 8.7mg/mL in DMSO

储存条件:4°C, protect from light

注意事项：

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References:

[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]