NSC12

製品コードS7940 バッチS794001

化学情報

	Synonyms	NSC 172285	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₄H₃₄F₆O₃
	分子量	484.52	CAS No.	102586-30-1
Solubility (25°C)*	体外	Ethanol	63 mg/mL (130.02 mM)
		DMSO	10.3 mg/mL (21.25 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	NSC12 (NSC 172285) is an orally available pan-FGF trap able to inhibit FGF2/FGFR interaction and endowed with promising antitumor activity.
in vitro	NSC12 inhibits FGF-dependent tumor growth, angiogenesis, and metastases. NSC12 does not affect FGF2/heparin interaction, whereas it inhibits the binding of FGF2 to the immobilized receptor (ID50 ∼30 μM). NSC12 interferes with FGF2/FGFR1 interaction without affecting the ability of the growth factor to interact with heparin or HSPGs. NSC12 also binds immobilized FGF3, FGF4, FGF6, FGF8, FGF16, FGF18, FGF20, and FGF22 with Kd values ranging between ∼16 and ∼120 μM. NSC12 may act as a multi-FGF trap by interacting with all members of the canonical FGF subfamilies. NSC12 hampers FGF23-mediated FGFR1 activation in Klotho-expressing Chinese hamster ovary (CHO) cells. Treatment with NSC12 causes the reduction of the S phase of the cell cycle in all tumor cell lines but LLC cells, in which an accumulation in the S phase is observed. NSC12 inhibits FGFR1, FGFR2, FGFR3, and FGFR4 phosphorylation in CHO cell transfectants. NSC12 inhibits the proliferation of various FGF-dependent murine and human cancer cell lines with no inhibitory effect on HCC827 cancer cells that harbor a tumor-driving mutation of the EGFR TK domain and on FGF-independent cancer cell lines^[1].
in vivo	Parenteral and oral delivery of NSC12 inhibits FGFR activation, tumor growth, angiogenesis, and metastasis in FGF-dependent murine and human tumor models. NSC12 causes a significant decrease of tumor weight, tumor cell FGFR1 phosphorylation and proliferation, and tumor CD31+ neovascularization at all the doses tested in the animal models^[1].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	KATO Ⅲ cells
	濃度	1.0 or 3.0 μM
	反応時間	72 h
	実験の流れ	KATO Ⅲ cells are plated at 10⁴ cells/well in 96 well-plates in RPMI medium plus 1% FBS. After 24 hr cells are treated with different FGFs (30 ng/ml) in the absence or presence of an optimal dose of NSC12 (1.0 or 3.0 μM) or NSC21. After 72 hr the MTT assay is performed according to manufacturer’s instructions. The optical density (OD) is determined using a plate reader at a test wavelength of 595 nm and a reference wavelength of 630 nm.
動物実験	動物モデル	C57BL/6 mice
	投薬量	from 2.5 to 10 mg/kg
	投与方法	i.p.

参考

[1] Ronca R, et al. Cancer Cell. 2015, 28(2):225-39.

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：

MiR-148b-3p inhibits renal carcinoma cell growth and pro-angiogenic phenotype of endothelial cell potentially by modulating FGF2. [Zhang H, et al. Biomed Pharmacother, 2018, 107:359-367]	PubMed: 30099339

MiR-148b-3p inhibits renal carcinoma cell growth and pro-angiogenic phenotype of endothelial cell potentially by modulating FGF2. [Zhang H, et al. Biomed Pharmacother, 2018, 107:359-367]

PubMed: 30099339

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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