SN-38 (86639-52-3) is the active metabolite of CPT-11 that inhibits DNA topoisomerase I (IC50 values are 0.74 and 1.9 μM in P388 and Ehrlich cells respectively). Inhibits DNA and RNA synthesis (IC50 values are 0.077 and 1.3 μM respectively) but does not affect protein synthesis. SN-38 displays potent antitumor activity against a range of human tumor cell lines (IC50 values are 3.3, 13, 19 and 22 nM for HCT-116, BEL-7402, HL60 and HeLa cells respectively). SN-38(86639-52-3)是CPT-11的活性代谢物,对DNA拓扑异构酶I具有抑制作用(P388和Ehrlich细胞的IC50值分别为0.74和1.9 μM)。 抑制DNA和RNA合成(IC50值分别为0.077和1.3 μM),但不影响蛋白质合成。 SN-38对一系列人类肿瘤细胞系显示出强大的抗肿瘤活性(对HCT-116、BEL-7402、HL60和HeLa细胞的IC50值分别为3.3、13、19和22 nM)。
References/Citations:
1) Koizumi et al. (2006), Novel SN-38-incorporating polymeric micelles, NKK012, eradicate vascular endothelial growth factor-secreting bulky tumors; Cancer Res., 66 10048 2) Gao et al. (2005), Synthesis and antitumor activity of the hexacyclic camptothecin derivatives; Bioorg. Med. Chem. Lett., 15 3233 3) Kawato et al. (1991), Intracellular roles of SN-38, a metabolite of the camptothecin derivative CPT-11, in the antitumor effect of CPT-11; Cancer Res., 51 4187
CAS:
86639-52-3
Catalog Number:
10-2425
Activity:
DNA topoisomerase I inhibitor
Chemical Name:
7-Ethyl-10-hydroxycamptothecin
Molecular Weight:
392.41
Molecular Formula:
C22H20N2O5 Solubility:
Soluble in DMSO (up to 40 mg/ml).
Physical Properties:
Off-white solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 1 month.
Shipping Code:
RT
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