Belotecan hydrochloride (CKD-602)

A DNA topoisomerase I inhibitor

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数量
5mg

￥1287.00

1030.00

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10mg

￥1937.00

1550.00

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25mg

￥2937.00

2350.00

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50mg

￥3887.00

3110.00

- +
100mg

￥5050.00

4040.00

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Background

Belotecan is an inhibitor of DNA topoisomerase I (IC₅₀ = 0.119 ?g/ml) and a derivative of the DNA topoisomerase I inhibitor camptothecin .¹ It inhibits the proliferation of various cancer cell lines, including KATO III stomach, HT-29 colon, A549 lung, MDA-MB-231 breast, and SKOV3 ovarian cancer cells (IC₅₀s = 160, 10.9, 9, 345, and 31 ng/ml, respectively). Belotecan (150 ng/ml) induces apoptosis and cell cycle arrest at the G₂/M phase in, and inhibits invasion of, SiHa cervical cancer cells.² It reduces tumor growth in a Ca Ski cervical cancer mouse xenograft model when administered at a dose of 25 mg/kg. Belotecan (80 ?g/kg) reduces food intake and body weight in pregnant dams and increases fetal deaths and decreases litter size.³ Formulations containing belotecan have been used in the treatment of ovarian and small cell lung cancer.

1.Lee, J.H., Lee, J.M., Kim, J.K., et al.Antitumor activity of 7-[2-(N-isopropylamino)ethyl]-(20S)-camptothecin, CKD602, as a potent DNA topoisomerase I inhibitorArch. Pharm. Res.21(5)581-590(1998) 2.Lee, S., Ho, J.Y., Liu, J.J., et al.CKD-602, a topoisomerase I inhibitor, induces apoptosis and cell-cycle arrest and inhibits invasion in cervical cancerMol. Med.25(1)23(2019) 3.Chung, M.-K., Kim, J.-C., and Han, S.-S.Embryotoxic effects of CKD-602, a new camptothecin anticancer agent, in ratsReprod. Toxicol.20(1)165-173(2005)

Protocol

Cell experiment:

The cells are treated with different concentrations (0.01, 0.1, 0.5, 1, 5 and 10 μg/mL) of belotecan for 24, 48 and 72 h. Control samples of each cell line are treated with medium only. Cell viability is measured using the MTS assay[1].

Animal experiment:

Mice: Nude mice with established U87MG glioma are treated with a dose of belotecan of 0 mg/kg (control group, injection with saline), 40 mg/kg (group A) or 60 mg/kg (group B). Thereafter, the dose is repeated once every 4 days for a total of four doses. Tumor volume is measured histologically and apoptosis is detected[1].

参考文献:

[1]. Kim YK, et al. Anticancer effects of CKD-602 (Camtobell?) via G2/M phase arrest in oral squamous cell carcinoma cell lines. Oncol Lett. 2015 Jan;9(1):136-142.
[2]. Kim YY, et al. CKD-602, a camptothecin derivative, inhibits proliferation and induces apoptosis in glioma cell lines. Oncol Rep. 2009 Jun;21(6):1413-9.
[3]. Kim CY, et al. Antitumor activity of CKD-602, a camptothecin derivative, in a mouse glioma model. J Clin Neurosci. 2012 Feb;19(2):301-5.