Tasisulam

製品コードS7326 バッチS732601

化学情報

	Synonyms	LY573636	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₁₁H₆BrCl₂NO₃S₂
	分子量	415.11	CAS No.	519055-62-0
Solubility (25°C)*	体外	DMSO	83 mg/mL (199.94 mM)
		Ethanol	83 mg/mL (199.94 mM)
		Water	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	Tasisulam (LY573636) is an antitumor agent and an apoptosis inducer via the intrinsic pathway. Phase 3.
in vitro	Tasisulam inhibits growth of various human leukemia and lymphoma cell lines with ED50 ranging from 7 to 40 μM. LY573636 also induces apoptosis in HL60, Reh, and MD901 cells, mainly by loss of mitochondrial membrane potential and induction of reactive oxygen species. ^[1] In addition, Tasisulam also produce antiproliferative activities in more than 70% of the 120 cell lines tested with EC50 of less than 50 μM. Tasisulam induces G2–M accumulation and subsequent apoptosis in Calu-6 and A-375 cells. In vitro, Tasisulam also inhibits VEGF-, FGF- and EGF-induced endothelial cord formation with EC50 of 47, 103, and 34 nM, respectively. ^[2]
in vivo	Tasisulam induces morphologic features of vascular normalization, including increased pericyte coverage and decreased hypoxia in vivo. Tasisulam (25 or 50 mg/kg, i.v.) displays dose-dependent antitumor activity, induces apoptosis, and normalizes tumor-associated vasculature in the Calu-6 non–small cell lung xenograft model. Besides, Tasisulam displays potent antitumor activity across a range of in vivo xenografts, including colorectal (HCT-116), melanoma (A-375), gastric (NUGC-3), leukemia (MV-4-11), and pancreatic (QGP-1). ^[2]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	B-cell acute lymphocytic leukemia (Reh, RCH, BALL1), Burkitt’s lymphoma (Daudi), diffuse large B-cell lymphoma (MD901, LY4), myeloid leukemia cell lines (HL60 and U937), Mantle cell lymphoma cell lines (NCEB1, Jeko1, and SP49).
	濃度	~40 μM
	反応時間	96 hours
	実験の流れ	Cells are treated with various concentrations of LY573636. 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay is performed. Briefly, MTT is dissolved in phosphate-buffered saline (PBS) at 5 mg/mL. Approximately 1,000 cells per well are incubated in culture medium for 96 hours in 96-well plates; and then, 10 μL of the MTT solution is added. After a 4-hour incubation, 100 μL of solubilization solution (20 % sodium dodecyl sulfate [SDS]) is added, and the mixture was incubated at 37 °C for 16 hours. In this assay, MTT is cleaved to an orange formazan dye by metabolically active cells; and the absorbance of the formazan product is measured with an enzyme-linked immunoabsorbent assay (ELISA) reader at 540 nm.
動物実験	動物モデル	Calu-6 non–small cell lung xenograft model
	投薬量	~50 mg/kg
	投与方法	i.v.

参考

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Synthesis of a Sulfonimidamide-Based Analog of Tasisulam and Its Biological Evaluation in the Melanoma Cell Lines SKMel23 and A375 [Steinkamp AD, et al. Skin Pharmacol Physiol, 2016, 29(6):281-290]	PubMed: 28013301

Synthesis of a Sulfonimidamide-Based Analog of Tasisulam and Its Biological Evaluation in the Melanoma Cell Lines SKMel23 and A375 [Steinkamp AD, et al. Skin Pharmacol Physiol, 2016, 29(6):281-290]

PubMed: 28013301

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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