SN 38 CAS: 86639-52-3
MF: C22H20N2O5
MW: 392.41

SN 38 (CAS 86639-52-3)

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SN 38 is rated 5.0 out of 5 by 3.
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別名: SN 38 is also known as NK 012.
アプリケーション: SN 38 is the active metabolite of the topoisomerase-I (topo-I) inhibitor Irinotecan (CPT-11), able to inhibit DNA topoisomerase I.
CAS 番号: 86639-52-3
Purity: ≥98%
Molecular Weight: 392.41
Molecular Formula: C22H20N2O5
補足情報: This is classified as a Dangerous Good for transport and may be subject to additional shipping charges.
試験・研究用以外には使用しないでください。 臨床及び体外診断には使用できません。
* Refer to Certificate of Analysis for lot specific data (including water content).

SN 38 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 is anctive metabolite of CPT-11 that inhibits DNA topoisomerase I (IC50 values are 0.74 and 1.9 μM in P388 and Ehrlich cells respectively). During hydrolysis, SN 38 is formed when the carboxylesterases metabolize irinotecan through glucuronidation by UDP glucuronosyl transferase 1A1. Compared to irinotecan, SN 38 is a more potent topoisomerase I inhibitor, and more cytotoxic to HT-29 colon cancer cells.


参考文献

1. Rothenberg, M.L.Topoisomerase I inhibitors: Review and update. Ann. Oncol. 8(9), 837-855 (1997).
2. Dancey, J., and Eisenhauer, E.A.Current perspectives on camptothecins in cancer treatment. Br. J. Cancer 74(3), 327-338 (1996).
3. Mathijssen, R.H.J., van Alphen, R.J., Verweij, J., et al.Clinical pharmacokinetics and metabolism of irinotecan (CPT-11). Clin. Cancer Res. 7(8), 2182-2194 (2001).
4. Ma, M.K., and McLeod, H.L.Lessons learned from the irinotecan metabolic pathway. Curr. Med. Chem. 10(1), 41-49 (2003).
5. 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.
6. Gao et al (2005) Synthesis and antitumor activity of the hexacyclic camptothecin derivatives. Bioorg.Med.Chem.Lett. 15 3233.
7. Koizumi et al (2006) Novel SN-38-incorporating ploymeric micelles, NK012, eradicate vascular endothelial growth factor-secreting bulky tumors. Cancer Res. 66 10048.

Physical State :
Solid
Solubility :
Soluble in DMSO (100 mM).
保存方法 :
Store at 4° C
Melting Point :
217° C (lit.)
Boiling Point :
~810.3° C at 760 mmHg (Predicted)
Density :
~1.5 g/cm3 (Predicted)
Refractive Index :
n20D 1.74 (Predicted)
Optical Activity :
α20D -19.2, c = 0.8 in DMSO; α20D +21.5±4.5, c = 0.2 in THF
IC50 :
HCT-116: IC50 = 3.3 nM (human); BEL-7402: IC50 = 13 nM (human); HL60: IC50 = 19 nM (human); HELA cell: IC50 = 22 nM (human); DNA synthesis: IC50 = 0.077 µM
Ki Data :
CYP3A4: Ki= 26 µM (human)
pK Values :
pKa: 9.13 (Predicted), pKb: 5.75 (Predicted)
試験・研究用以外には使用しないでください。 臨床及び体外診断には使用できません。
WGK Germany :
3
RTECS :
UQ0491000
PubChem CID :
MDL Number :
MFCD06762720
SMILES :
CCC1=C2C=C(C=CC2=NC3=C1CN4C3=CC5=C(C4=O)COC(=O)C5(CC)O)O

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SN 38 (CAS 86639-52-3)  参考文献

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引用 1 to 10 of 17 合計

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PMID: # 33535454  Park, R.|Park, EJ.|Cho, YY.|Lee, JY.|Kang, HC.|Song, IS.|Lee, HS.| et al. 2021. Pharmaceutics. 13:

PMID: # 31430908  Kim, S. et al. 2019. Molecules. 24:

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PMID: # 27128896  Kwon, SS. et al. 2016. Molecules. 21:

PMID: # 27825129  Li, DD. et al. 2016. Oncotarget. 7: 80842-80854.

PMID: # 25522350  Joo, J. et al. 2015. Biopharm Drug Dispos. 36: 258-64.

PMID: # 25904760  Lee, B. et al. 2015. Drug Metab. Dispos. 43: 1137-46.

引用 1 to 10 of 17 合計
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