(S)-10-Hydroxycamptothecin


CAS No. : 19685-09-7

(S)-10-Hydroxycamptothecin,19685-09-7
Product Details
For research use only. Not Intended for Therapeutic Use!
Cat No:I002507
Synonyms:(S)-4-ethyl-4,9-dihydroxy-1H-pyrano[3/',4/':6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione
Molecular Formula:C20H16N2O5
Molecular Weight:364.4
Target:Topoisomerase
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Appearance:Light yellow solid powder
Purity: > 98%
Cat No:I002507
Cas No:19685-09-7
Product-Name:(S)-10-Hydroxycamptothecin
InChI:InChI=1S/C20H16N2O5/c1-2-20(26)14-7-16-17-11(5-10-6-12(23)3-4-15(10)21-17)8-22(16)18(24)13(14)9-27-19(20)25/h3-7,23,26H,2,8-9H2,1H3/t20-/m0/s1
InChIKey:HAWSQZCWOQZXHI-FQEVSTJZSA-N
SMILES:O=C([C@]1(O)CC)OCC2=C1C=C(C(N=C(C=CC(O)=C3)C3=C4)=C4C5)N5C2=O

(S)-10-Hydroxycamptothecin is a clinical therapy agent against hepatoma.
IC50 value:
Target:
In vitro: In vitro, the 10-hydroxycamptothecin nanosuspensions released the encapsulated drug with nearly zero-order kinetics, and the accumulative release reached 90% within 72 hours. In vitro cytotoxicity assay showed that the 10-hydroxycamptothecin nanosuspensions had significantly enhanced cytotoxicity against HepG2 cells compared to the commercially available 10-hydroxycamptothecin injections [1].
In vivo: The in vivo study with H22 tumor-bearing mice and intravenous injection of the drug showed that in contrast to the 10-hydroxycamptothecin injections, the 10-hydroxycamptothecin nanosuspensions exhibited significantly enhanced biodistribution, particularly in the lung (393.40-fold AUC0–24 h, liver (192.35-fold AUC0–24 h, spleen (141.67-fold AUC0–24 h and tumor (64.21-fold AUC0–24 h. The 10-hydroxycamptothecin nanosuspensions also showed improved antitumor therapeutic efficacy over the injections (89.83% vs. 30.56%) [1].


1:Combination treatment with Rhizoma Paridis and Rhizoma Curcuma longa extracts and 10-hydroxycamptothecin enhances the antitumor effect in H22 tumor model by increasing the plasma concentration. Liu Z, Li H, Fan Y, Liu Y, Man S, Yu P, Gao W.Biomed Pharmacother. 2016 Oct;83:627-634. doi: 10.1016/j.biopha.2016.07.026. Epub 2016 Jul 25. PMID: 27459119
2:Effects of nanoparticle size on antitumor activity of 10-hydroxycamptothecin-conjugated gold nanoparticles: in vitro and in vivo studies. Bao H, Zhang Q, Xu H, Yan Z.Int J Nanomedicine. 2016 Mar 7;11:929-40. doi: 10.2147/IJN.S96422. eCollection 2016. PMID: 27022260 Free PMC Article
3:Effects of 10-hydroxycamptothecin on intrinsic mitochondrial pathway in silkworm BmN-SWU1 cells. Pan C, Hu YF, Song J, Yi HS, Wang L, Yang YY, Wang YP, Zhang M, Pan MH, Lu C.Pestic Biochem Physiol. 2016 Feb;127:15-20. doi: 10.1016/j.pestbp.2015.09.001. Epub 2015 Sep 3. PMID: 26821653
4:In vitro and in vivo anti-tumor efficacy of 10-hydroxycamptothecin polymorphic nanoparticle dispersions: shape- and polymorph-dependent cytotoxicity and delivery of 10-hydroxycamptothecin to cancer cells. Wang H, Feng J, Liu G, Chen B, Jiang Y, Xie Q.Nanomedicine. 2016 May;12(4):881-91. doi: 10.1016/j.nano.2015.12.373. Epub 2016 Jan 6. PMID: 26767513
5:Hyaluronic Acid Modified Hollow Prussian Blue Nanoparticles Loading 10-hydroxycamptothecin for Targeting Thermochemotherapy of Cancer. Jing L, Shao S, Wang Y, Yang Y, Yue X, Dai Z.Theranostics. 2016 Jan 1;6(1):40-53. doi: 10.7150/thno.13250. eCollection 2016. PMID: 26722372 Free PMC Article
6:Liposomes Encapsulating 10-Hydroxycamptothecin-Cyclodextrin Complexes and Their In Vitro Anti-Tumor Activities. Chen Y, Chen C, Xiao Y, Zhang X, Chen Y.J Nanosci Nanotechnol. 2015 May;15(5):3786-95. PMID: 26505006
7:Intracellular delivery of 10-hydroxycamptothecin with targeted nanostructured lipid carriers against multidrug resistance. Liu M, Chen D, Mukerabigwi JF, Chen S, Zhang Y, Lei S, Luo S, Wen Z, Cao Y, Huang X, He H.J Drug Target. 2016;24(5):433-40. doi: 10.3109/1061186X.2015.1086358. Epub 2015 Sep 30. PMID: 26422582
8:A novel drug-polyethylene glycol liquid compound method to prepare 10-hydroxycamptothecin loaded human serum albumin nanoparticle. Yang Z, Gong W, Wang Z, Li B, Li M, Xie X, Zhang H, Yang Y, Li Z, Li Y, Yu F, Mei X.Int J Pharm. 2015 Jul 25;490(1-2):412-28. doi: 10.1016/j.ijpharm.2015.05.073. Epub 2015 May 28. PMID: 26027489
9:Synthesis and Biological Evaluation of Novel Water-Soluble Poly-(ethylene glycol)-10-hydroxycamptothecin Conjugates. Guo N, Jiang D, Wang L, You X, Teng YO, Yu P.Molecules. 2015 May 21;20(5):9393-404. doi: 10.3390/molecules20059393. PMID: 26007190 Free Article
10:RPL13A as a reference gene for normalizing mRNA transcription of ovarian cancer cells with paclitaxel and 10-hydroxycamptothecin treatments. Bian Z, Yu Y, Quan C, Guan R, Jin Y, Wu J, Xu L, Chen F, Bai J, Sun W, Fu S.Mol Med Rep. 2015 Apr;11(4):3188-94. doi: 10.3892/mmr.2014.3108. Epub 2014 Dec 17. PMID: 25523336
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