BMS-1001

製品コードS9610 バッチS961003

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder
	化学式	C₃₅H₃₄N₂O₇
	分子量	594.65	CAS No.	2113650-03-4
Solubility (25°C)*	体外	DMSO	50 mg/mL warmed with 50ºC water bath (84.08 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	BMS-1001 is a potent inhibitor of PD-1/PD-L1 interaction with EC50 of 253 nM. BMS-1001 alleviates the inhibitory effect of the soluble PD-L1 on the T-cell receptor-mediated activation of T-lymphocytes.
in vitro	BMS-1001 alleviates the inhibitory effect of the soluble PD-L1 on the T-cell receptor-mediated activation of T-lymphocytes. BMS-1001 is effective in attenuating the inhibitory effect of the cell surface-associated PD-L1.^[1]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	PD-L1⁺ aAPC/CHO-K1 cells (aAPCs), PD-1 Effector Cells (ECs)
	濃度	0.12 μM, 0.3 μM, 1.2 μM, 3 μM
	反応時間	24 h
	実験の流れ	For the evaluation of the BMS impact on T cell inhibition by soluble PD-L1, the ECs are stimulated with the anti-CD3 antibody in the presence of the recombinant human sPD-L1. For this, the 96-well white flat bottom plates are coated overnight at 4°C with 5 μg/ml of the anti-CD3 antibody or the isotype control solution in PBS. The antibody solution is removed and the plates are washed 3 times with PBS and dried. sPD-L1 (aa 18–134) is diluted in PBS supplemented with the penicillin/streptomycin solution (100 U/ml final concentration each) in the presence of the BMS-1001 or a corresponding volume of DMSO. Then, 15 μl of the solution is added to each well of the antibodycoated plate. ECs are centrifuged and diluted to 50 000 per ml, and 60 μl of the cell solution is added to each well. The final concentration of sPD-L1 was 10 μg/ml (0.6 μM). The final concentrations of BMS-1001 are: 0.12, 0.3, 1.2 and 3 μM, giving the following BMS:sPD-L1 molar ratios: 1:5, 1:2, 2:1 and 5:1. The cells are cultured for 24 h and the luciferase activity assay is performed using the Bio-Glo Luciferase Assay System.

参考

[1] Lukasz Skalniak, et al. Oncotarget. 2017 Aug 7;8(42):72167-72181.

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