Belotecan

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Belotecan

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

256411-32-2

CKD-602 free base

Belotecan (CKD-602 free base) 是DNA topoisomerase I抑制剂。Belotecan 诱导细胞凋亡以及周期阻滞。Belotecan 是一种具有抗肿瘤效应的喜树碱衍生物，可用于癌症的研究。

生物活性

Belotecan (CKD-602 free base) is aDNAtopoisomeraseIinhibitor. Belotecan induces cellapoptosisand cell-cycle arrest. Belotecan is a camptothecin analogue with anti-tumor effects, it can be used for the research ofcancer^[1].

IC₅₀& Target

IC50: 30 ng/mL (Caski cells), 150 ng/mL (HeLa cells), 150 ng/mL (SiHa cells)^[1]

体外研究
(In Vitro)

Belotecan (0-600 ng/mL; 0-72 h) time- and dose-dependently inhibits viability of Caski cells, HeLa cells and SiHa cells at 48 h with IC₅₀values of 30, 150 and 150 ng/mL, respectively^[1].
Belotecan (0-150 ng/mL; 48 h) induces cell apoptosis and cell-cycle arrest, and affects PARP, cleaved PARP, BAX, p53, Ser15, cell cycle related protein expression and cancer invasion in cervical cancer^[1].

Apoptosis Analysis^[1]

Cell Line:	Caski, HeLa and SiHa cell lines
Concentration:	0-150 ng/mL
Incubation Time:	48 h
Result:	Showed strong pro-apoptotic activities to Caski, HeLa and SiHa cells.

Western Blot Analysis^[1]

Cell Line:	Caski, HeLa and SiHa cell lines
Concentration:	0-150 ng/mL
Incubation Time:	48 h
Result:	Increased the expression of PARP, cleaved PARP, BAX, p53, Ser15, cyclin B1, phosphorylated cyclin B1 and phospho-cdc2 (Tyr15) protein, and decreased MMP2 and VEGF protein expression.

Cell Cycle Analysis^[1]

Cell Line:	Caski, HeLa and SiHa cell lines
Concentration:	0-150 ng/mL
Incubation Time:	48 h
Result:	Induced cell-cycle arrest in the G2/M phase in cervical cancer.

Cell Invasion Assay^[1]

Cell Line:	Caski, HeLa and SiHa cell lines
Concentration:	0-150 ng/mL
Incubation Time:	48 h
Result:	Inhibited cancer invasion in cervical cancer.

体内研究
(In Vivo)

Belotecan (25 mg/kg; i.v. for 16 days at 4-day intervals) inhibits tumor growth in CaSki-xenografts nude mice^[1].

Animal Model:	BALB/c-nude mice with CaSki cells injection^[1]
Dosage:	25 mg/kg
Administration:	Intravenous injection; 25 mg/kg; 16 days at 4-day intervals
Result:	Significantly inhibited the tumor growth and showed no significant difference in bodyweight of xenograft mice and the controls.

Clinical Trial

分子量

433.50

Formula

C₂₅H₂₇N₃O₄

CAS 号

256411-32-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.