Topotecan HCl

製品コードS1231 バッチS123105

化学情報

	Synonyms	Nogitecan HCl, SKFS 104864A, NSC 609699	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₃H₂₃N₃O₅.HCl
	分子量	457.91	CAS No.	119413-54-6
Solubility (25°C)*	体外	DMSO	92 mg/mL (200.91 mM)
		Water	92 mg/mL (200.91 mM)
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Topotecan HCl is a topoisomerase I inhibitor for MCF-7 Luc cells and DU-145 Luc cells with IC50 of 13 nM and 2 nM in cell-free assays, respectively. Topotecan HCl induces autophagy and apoptosis.
in vitro	Stronger drug activity of Topotecan is observed for DU-145 Luc and MCF-7 Luc cells. ^[1] Topotecan causes cytotoxicity during the course of DNA replication by stabilizing the covalent complex between topoisomerase I and DNA and preventing the religation of enzyme-linked single-strand DNA break. Topotecan stabilizes topoisomerase I/DNA cleavable complexes in radiation-resistant human B-lineage acute lymphoblastic leukemia (ALL) cells, causes rapid apoptotic cell death despite high-level expression of bcl-2 protein, and inhibits ALL cell clonogenic growth in a dose-dependent fashion. ^[2]
in vivo	Animals inoculate s.c. with DU-145 Luc cells and then treated with Topotecan demonstrates significant tumor growth and regression as measured with calipers and luminescent imaging. The correlation coefficient is 0.75 for the control untreated group and 0.93 for the Topotecan-treated group. Similarly, tumor progression and regression are measurable using luminescent imaging for untreated and Topotecan-treated mice inoculated i.p. with MCF-7 Luc cells. ^[1] Topotecan elicited potent antileukemic activity in severe combined immune-deficiency (SCID) mouse models of human poor prognosis ALL. Topotecan markedly improved event-free survival of SCID mice challenged with otherwise fatal doses of humaln leukemia cells at systemic drug exposure levels. ^[2] Gliomas preferentially express TRAIL R2 and that treatment with Topotecan significantly up-regulates its expression. ^[3]
特徴	Topotecan is a water-soluble derivative of camptothecin.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	MCF-7 Luc and DU-145 Luc cells
	濃度	0 μg/mL - 0.692 μg/mL
	反応時間	96 hours
	実験の流れ	Topotecan is dissolved in sterile water to a stock concentration of 1 mg/mL, diluted to 6 μg/mL in cultured medium and then serially diluted 1:4 in opaque, white tissue culture-treated microplates to a final volume of 0.1 mL/well. MCF-7 Luc and DU-145 Luc cells are resuspended in 3×10⁴ cells/mL in DMEM with high glucose containing 10% FBS and 0.5 mg/mL Geneticin; 100 μL of cells are added in each well. Plates are incubated for 4 days at 37 °C in 95% humidity/5% CO₂. After incubation, 0.05 mL of 0.1 M HEPES buffer (pH 7.9) containing 50 μg/mL D-luciferin is added to each well. After incubation at room temperature for 10 minutes, the culture microplate is measured in a microplate luminometer and a molecular light imager. Results obtained with the microplate luminometer are calculated using no inhibition control wells without exogenous drug and maximum inhibition control wells containing ATP inhibitor. Results for the molecular light imager are similarly calculated using values obtained with a 5 minutes luminescent imager.
動物実験	動物モデル	Mice with MCF-7 Luc or DU-145 Luc cells
	投薬量	0.25 mg/mL
	投与方法	Administered via i.p.

参考

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カスタマーフィードバック

: Data from [Data independently produced by PLoS Genet, 2014, 10(1), e1004107]

: Data from [Data independently produced by , , BMC Cancer, 2015, 10.1186/s12885-015-1231-z]

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長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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