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(s)-10-hydroxycamptothecin

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Chemical Structure| 19685-09-7 同义名 : 10-羟基喜树碱 ;10-HCPT;ChEMBL 273862;10-hydroxycamptothecine;Hydroxycamptothecin;10-OHCPT;NSC 107124;10-Hydroxycamptothecin
CAS号 : 19685-09-7
货号 : A155153
分子式 : C20H16N2O5
纯度 : 98+%
分子量 : 364.351
MDL号 : MFCD02093100
存储条件：

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(137.23 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

30% PEG400+0.5% Tween80+5% propylene glycol+water 30 mg/mL suspension

生物活性
靶点

  • Topo I
描述 (S) -10-Hydroxycamptothecin (HCPT) is a TOP I (Topoisomerase I) specific inhibitor. HCPT inhibits the growth of ESCC cells in vitro and verify its anti-tumor activity in vivo by using a patient-derived xenograft (PDX) tumor model in mice. HCPT also induced DNA damage by increasing the expression of H2A.XS139. HCPT significantly decreased the proliferation and anchorage-independent growth of ESCC (Esophageal squamous cell carcinoma) cells (KYSE410, KYSE510, KYSE30, and KYSE450). Mechanistically, HCPT inhibited the G2/M phase cell cycle transition, decreased the expression of cyclin B1, and elevated p21 expression. In addition, HCPT stimulated ESCC cells apoptosis, which was associated with elevated expression of cleaved PARP, cleaved caspase-3, cleaved caspase-7, Bax, Bim, and inhibition of Bcl-2 expression. HCPT dramatically suppressed PDX tumor growth and decreased the expression of Ki-67 and TOP I and increased the level of cleaved caspase-3 and H2A.XS139 expression. HCPT inhibited ESCC growth, arrested cell cycle progression, and induced apoptosis both in vitro and in vivo via decreasing the expression and activity of TOP I enzyme[3]. HCPT may induce fibroblast apoptosis by regulating miR‑23b‑3p expression[4].(S)-10-Hydroxycamptothecin (OPT), an analog of camptothecin (CPT), was found to inhibit the growth of the mouse hepatoma BW7756, when given at 1.0 mg/kg/day for 14 days. This drug inhibited the S-Phase of the tumor cells in vivo and the S and G2/M phases in vitro[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.74mL

0.55mL

0.27mL

13.72mL

2.74mL

1.37mL

27.45mL

5.49mL

2.74mL
参考文献

[1]Ping YH, Lee HC, et al. Anticancer effects of low-dose 10-hydroxycamptothecin in human colon cancer. Oncol Rep. 2006 May;15(5):1273-9.

[2]Vladu B, Woynarowski JM, et al. 7- and 10-substituted camptothecins: dependence of topoisomerase I-DNA cleavable complex formation and stability on the 7- and 10-substituents. Mol Pharmacol. 2000 Feb;57(2):243-51.

[3]Song M, Yin S, Zhao R, Liu K, Kundu JK, Shim JH, Lee MH, Dong Z. (S)-10-Hydroxycamptothecin Inhibits Esophageal Squamous Cell Carcinoma Growth In Vitro and In Vivo Via Decreasing Topoisomerase I Enzyme Activity. Cancers (Basel). 2019 Dec 6;11(12):1964

[4]Zeng L, Sun Y, Li X, Wang J, Yan L. 10 Hydroxycamptothecin induces apoptosis in human fibroblasts by regulating miRNA 23b 3p expression. Mol Med Rep. 2019 Apr;19(4):2680-2686

[5]Tsou KC, Xu B, Miller EE, Lo KW. Anti-tumor effect of (S)-10-hydroxycamptothecin on mouse hepatoma BW7756 and its possible mode of action. Anticancer Res. 1981;1(2):115-9