Belotecan hydrochloride(CKD-602)

Cas No.:	213819-48-8
Chemical Name:	Belotecan hydrochloride
Synonyms:	Camtobell hydrochloride;(S)-4-Ethyl-4-hydroxy-11-[2-(isopropylamino)ethyl]-3,4,12,14-tetrahydro-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14-dione hydrochloride;Belotecan Hydrochloride;CKD-602;Belotecan HCl;CKD 602;Belotecan (hydrochloride);01DZ4127G7;Belotecan hydrochloride (USAN);Belotecan Hydrochloride [USAN];BCP28717;API0009359;D03225;819C488;7-(2-(N
SMILES:	Cl[H].O1C([C@](C([H])([H])C([H])([H])[H])(C2C([H])=C3C4C(=C(C5=C([H])C([H])=C([H])C([H])=C5N=4)C([H])([H])C([H])([H])N([H])C([H])(C([H])([H])[H])C([H])([H])[H])C([H])([H])N3C(C=2C1([H])[H])=O)O[H])=O
Formula:	C25H28ClN3O4
M.Wt:	469.9605
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	Belotecan hydrochloride (CKD-602 hydrochloride), a Topoisomerase I inhibitor, is a synthetic and water-soluble camptothecin derivative.
In Vivo:	Belotecan has a significant effect on intracerebral glioma growth, with animals having significantly smaller tumors than those in the control group[3].
In Vitro:	Belotecan exerts a significant cytotoxic effect on YD-8, YD-9 and YD-38 cells in a time- and dose-dependent manner with IC50 values of 2.4, 0.18 and 0.05 μg/mL at 72 h following treatment. Belotecan induces apoptosis in these cell lines. Belotecan induces G2/M phase arrest in oral squamous cell cancer cells[1]. Belotecan shows a significant anticancer effect on glioma cells, with IC50 values of 9.07 nM for LN229, 14.57 nM for U251 MG, 29.13 nM for U343 MG, and 84.66 nM for U87 MG[2].
Cell Assay:	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 Administration:	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].
References:	[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.