CZ415

製品コードS8298 バッチS829801

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₂H₂₉N₅O₄S
	分子量	459.56	CAS No.	1429639-50-8
Solubility (25°C)*	体外	DMSO	91 mg/mL (198.01 mM)
		Water	Insoluble
		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	CZ415, a potent ATP-competitive mTOR inhibitor with very good cell permeability.
in vitro	CZ415 shows no genotoxic potential and has very good cell permeability. Treatment of CZ415 leads to inhibition of phosphorylation for downstream targets of mTORC1 and mTORC2(IC50=14.5 nM for pS6RP and IC50=14.8 nM for pAKT). The immunosuppressive effect of CZ415 is measured by detecting secreted IFNγ after 18 h in stimulated human whole blood, and the resulting IC50 was 226 nM. CZ415 shows no genotoxic potential. It is neither mutagenic in a bacterial mutation assay (Ames test) nor does it show genotoxicity in the mouse lymphoma assay (MLA), in either the presence or absence of rat-liver S9 mix^[1].
in vivo	In vivo studies show that CZ415 has moderate clearance and good oral bioavailability. In an anti-CD3 mouse model CZ415 efficiently inhibits mTOR downstream signaling and, in a CIA mouse model, shows significant antiinflammatory effects. With its extraordinary selectivity, drug-like properties and proven efficacy in vivo, CZ415 represents an ideal molecule for the pharmacological investigation of mTOR pathophysiological role in vivo^[1].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	HEK294T17 cells
	濃度	3 µM start, 8 points 1:3 dilution steps.
	反応時間	2 h
	実験の流れ	Cells are seeded in 90 µL DMEM containing 2% FCS at 4x10_⁴ cells/well (for pS6RP S240/244 assay) or 8x10_⁴ cells/well (for pAKT S473 assay) in a 96well U-bottom plate. The plate is then incubated for 1h in a humidified incubator (37ºC, 5% CO2) to allow cells to adhere. CZ415: 3 µM start, 8 points 1:3 dilution steps, n=2. Positive control: 1 μM PI-103 (n=8). Negative control: DMSO (n=8). 10 µL of 10x compound concentration in 1% DMSO/99% (DMEM 2% FCS) are added to the cells followed by 2 h incubation in a humidified incubator (37ºC, 5% CO2). Cells are lysed by addition of 10 μL 5x Complete Lysis Buffer and gentle shaking at 4°C for 15 min
動物実験	動物モデル	Male SD rats
	投薬量	1 mg/kg
	投与方法	i.v.

参考

[1] Cansfield AD, et al. ACS Med Chem Lett. 2016, 7(8):768-73.

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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