喜樹(shù)堿是拓撲異構酶I的選擇性抑制劑，IC50值為679 nM [1]。

喜樹(shù)堿可以誘導SMMC-7721、MCF-7和HCT-116腫瘤細胞的死亡。據報道，喜樹(shù)堿通過(guò)AMPK-TSC2-mTOR途徑誘導自噬，同時(shí)通過(guò)ATM-Chk2-p53-p21途徑誘導早衰[2]。 研究表明喜樹(shù)堿在非小細胞肺癌異種移植物中具有抗腫瘤活性。已經(jīng)發(fā)現喜樹(shù)堿誘導的DNA損傷導致H2AX (γH2AX)的磷酸化。以前的研究也證明了在用喜樹(shù)堿治療的癌細胞中減少Top1的表達[3]。

產(chǎn)品性質(zhì)：

Cas No.:7689-03-4

別名:喜樹(shù)堿; Campathecin; (S)-(+)-Camptothecin; CPT

化學(xué)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

儲存條件:4°C, protect from light

注意事項：

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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]