XAV939 - CAS:284028-89-3 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	XAV939 促销
英文名称:	XAV939
别名:	3,5,7,8-Tetrahydro-2-[4-(trifluoromethyl)phenyl]-4H-thiopyrano[4,3-d]pyrimidin-4-one
CAS No:	284028-89-3	分子式:	C₁₄H₁₁F₃N₂Os	分子量:	312.31
CAS No:	284028-89-3
分子式:	C₁₄H₁₁F₃N₂Os
分子量:	312.31
MDL:	MFCD16879017

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X10005 XAV939 ≥98%（HPLC） (psaitong)

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熔点：

207.14°C

包装规格：

5mg 25mg 100mg in glass bottle

溶解性：

溶于PBS (pH 7.2) 、(~0.15 mg/ml)、DMSO (~2 mg/ml)、DMF (~5 mg/ml)、水(<1 mg/ml at 25°C）和乙醇 (<1 mg/ml at 25 °C）.

产品描述：

基本信息

产品编号：X10005
产品名称：XAV939
CAS:	284028-89-3	储存条件	粉末	-20℃	四年

分子式：	C14H11F3N2Os		溶于液体	-80℃	两年
分子量	312.31			-20℃	一个月
化学名：	3,5,7,8-Tetrahydro-2-[4-(trifluoromethyl)phenyl]-4H-thiopyrano[4,3-d]pyrimidin-4-one
Solubility (25°C)	体外	DMSO	12mg/mL (38.42mM)
		Ethanol	Insoluble
		Water	Insoluble
	体内（现配现用）	4% DMSO+corn oil	1mg/mL
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。

制备储备液

浓度溶液体积质量	1mg	5mg	10mg
1mM	3.2019mL	16.0097mL	32.0195mL
5mM	0.6404mL	3.2019mL	6.4039mL
10mM	0.3202mL	1.6010mL	3.2019mL

生物活性

产品描述	有效的 tankyrase 抑制剂，靶向 Wnt/β-catenin 途径。
靶点/IC₅₀	TNKS2 (Cell-free assay) 4nM	TNKS1 (Cell-free assay) 11nM
体外研究	XAV939 also binds to recombinant PARP1, although with a significantly lower binding affinity (Kd=1.2μM). XAV939 (1μM) strongly inhibis STF activity in SW480 cells, Wnt3a-stimulated STF activity in HEK293 cells, but does not affect CRE, NF-κB or TGF-β luciferase reporters. XAV939 regulates axin levels through tankyrase inhibition in HEK293 cell[1]. XAV939 (0.5μM, 1.0μM) reduces DNA-PKcs protein levels 50% of the relative DMSO control in human lymphoblasts. XAV939 induces a second wave of pro-cardiomyocyte gene expression as shown by increased Mesp1 and Isl1expression 2 to 4 days after Wnt inhibition, and by increased Nkx2.5 expression 4 to 6 days after XAV939 addition. XAV-939 (10nM) has a suppressive effect on elevated MMP-13 levels in both IL-1β-induced SW 1353 cells.
体内研究	XAV-939 (3mL, 10nM) has a suppressive effect on elevated MMP-13 levels in the rat OA model. XAV-939 (1mg/mL, i.p.) ameliorates the psoriasiform skin disease induced by IMQ. XAV-939 results in a significant decrease in the IMQ-induced epidermal hyperplasia (indicated by acanthosis) and dermal inflammatory infiltrates in mice.

推荐实验方法(仅供参考)

激酶实验：

Kinase Assay

To assess the effect of compounds on auto-PARsylation of TNKS, 1μM GST fusion protein containing the SAM domain and the PARP domain of TNKS2 (a.a. 872-1166) is mixed with 5μM biotin-NAD+ and 2μM XAV939 or LDW643 at 30°C for 2.5 hours.Samples are resolved by SDS-PAGE and probed with streptavidin AlexaFluor680. To assess PARsylation of axin, recombinant full-length TNKS2 (expressed/purified as a N-terminal His-tagged protein in bacteria) is incubated with GST-axin 1 (1-280) in the presence of biotin-NAD+ with or without XAV939. The products are resolved and probed with Streptavidin-HRP and imaged using a AlphaInnotech imager. To assess the effect of XAV939, IWR-1-enod, IWR-1-exo, and ABT-888 on autoPARsylation of TNKS2, His-tagged full-length TNKS2 is incubated with 5μM biotin-NAD+ and 3mM of indicated compounds.The products are resolved and probed with Streptavidin-HRP. LC/MS-based high throughput auto-PARsylation assays for PARP1, PARP2, TNKS1, and TNKS2 are setup to monitor the formation of nicotinamide (a by-product of the PARsylation reaction) in the presence of small molecule inhibitors.

细胞实验:

Cell Assay

Human SW 1353 chondrosarcoma cells are seeded in 96-well plates (1×104 cells/well) and are treated with Icariin (0, 5, 10, 20, 40, 80, or 100μM). After 24 h, 20μL MTT (5mg/mL in PBS) is added to each well and plates are incubated at 37°C for another 4h. Supernatants are then removed, and 150μL DMSO is added to each well. After plates are shaken for 10 min,optical density values measured at 570nm are recorded using an ELISA reader.

动物实验:

Animal Administration

C57BL/6J mice are kept under specific pathogen-free conditions. XAV-939 is injected i.p., at a dose of 1mg/mL, once a day for seven consecutive days of IMQ treatment (injection volume 100μL). Control mice are injected with 100μL 10% DMSO/90% 0.9% NaCl, the solvent for XAV-939. To ameliorate any suffering of mice observed throughout these experimental studies, they are euthanized by CO2 inhalation.

保存条件：

-20℃

UN码：

HazardClass：

危害声明：

安全说明：

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