ND646

製品コードS8377 バッチS837701

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder
	化学式	C₂₈H₃₂N₄O₇S
	分子量	568.64	CAS No.	1434639-57-2
Solubility (25°C)*	体外	DMSO	100 mg/mL (175.85 mM)
		Ethanol	100 mg/mL (175.85 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	ND-646 is an allosteric inhibitor of the ACC (Acetyl-coA carboxylase) enzymes that prevents ACC subunit dimerization to suppress fatty acid synthesis with IC50 of 3.5 nM and 4.1 nM for hACC1 and hACC2, respectively.
in vitro	ND-646 inhibits FASyn in vitro and induces apoptosis in NSCLC cells. AMPK phosphorylation sites can be used as a biomarker to monitor ACC engagement by ND-646.^[1]
in vivo	Chronic ND-646 treatment of xenograft and genetically engineered mouse models of NSCLC inhibits tumor growth. When administered as a single agent or in combination with the standard-of-care drug carboplatin, ND-646 markedly suppresses lung tumor growth in the Kras;Trp53−/− (also known as KRAS p53) and Kras;Stk11−/− (also known as KRAS Lkb1) mouse models of NSCLC.^[1]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	A549 cells
	濃度	7 nM, 21 nM, 62 nM, 185 nM, 555 nM, 1666 nM, 5000 nM
	反応時間	24 hrs
	実験の流れ	All cell lines are incubated at 37 ℃ and are maintained in an atmosphere containing 5% CO2. A549, H460, H157 and H1355 cells are purchased from the ATCC. Cells are tested for Mycoplasma using manufacturer's conditions and are deemed negative. Cells are grown in Dulbecco's modified Eagles medium (DMEM) plus 10% fetal bovine serum. ACC1-KO clones are maintained in 10% FBS + addition of 200 μM palmitate every 3 days. For proliferation assays via cell counts, cells are plated into 24 well plates in triplicate at 2^E4 cells/well and the following day treated with either DMSO vehicle or ND-646. Cell counts are recorded at days 1, 3, 5 and 7-post treatment. For delipidated media, cells are first seeded in media containing regular 10% FBS and the following day are switched into media containing 20% delipidated FBS upon treatment. Viability assays are performed using either a WST-1 viability assay or Cyquant in 96 well culture plates under manufacturers conditions. For quantitation, values from treated cells are divided by values from control treated cells and expressed as percent control. Palmitate rescue experiments are performed in delipidated media by co-treating cells, in 24 well plates, with ND-646 and 200 μM of palmitate conjugated to BSA. For palmitate-BSA preparation, palmitate is solubilized in 100% Etoh @ 50 mM and combined with 4% fatty acid free BSA in saline at a ratio of 1:4 to make a palmitate concentration of 10 mM. Palmitate-BSA is used at a final concentration of 200 μM.
動物実験	動物モデル	female athymic nude mice
	投薬量	25 mg/kg, 50 mg/kg
	投与方法	Oral gavage

参考

[1] Robert U Svensson, et al. Nat Med. 2016 Oct;22(10):1108-1119.

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：

Dysregulated Lipid Synthesis by Oncogenic IDH1 Mutation Is a Targetable Synthetic Lethal Vulnerability [ Cancer Discov, 2023, 13(2):496-515]	PubMed: 36355448
A subset of VEGFR-TKIs activates AMPK in LKB1-mutant lung cancer [ Cancer Sci, 2023, 114(4):1651-1662]	PubMed: 36459496

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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