AX20017 - CAS:329221-38-7 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	AX20017
英文名称:	AX20017
别名:	PnG Inhibitor;2-(Cyclopropanecarbonylaino)-2,3,3a,4,5,6,7,7a-octahydro-1-benzothiophene-3-carboxaide
CAS No:	329221-38-7	分子式:	C₁₃H₂₀N₂O₂S	分子量:	268.37
CAS No:	329221-38-7
分子式:	C₁₃H₂₀N₂O₂S
分子量:	268.37

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A10994 AX20017 ≥98% (psaitong)

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包装规格：

5mg 25mg 100mg in glass bottle

溶解性：

溶于DMSO(≥30mg/mL ) -20°C 5mg 25mg 100mg in glass bottle

产品描述：

基本信息

产品编号：A10994
产品名称：AX20017
CAS:	329221-38-7	储存条件	粉末	-20℃	四年

分子式：	C13H20N2O2S		溶于液体	-80℃	六个月
分子量	268.37			-20℃	一个月
化学名：	2-[(cyclopropylcarbonyl)amino]-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxamide
Solubility (25°C)	体外	DMSO	100mg/mL (372.62mM)
		Ethanol
		Water
	体内	现配现用
＜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	3.7830mL	18.9150mL	37.8301mL
5mM	0.7566mL	3.7830mL	7.5660mL
10mM	0.3783mL	1.8915mL	3.7830mL

生物活性

产品描述	一种蛋白激酶G(PnG)抑制剂，IC50：0.39μ。
靶点/IC₅₀	PknG IC50: 0.39μM
体外研究	The compound AX20017 inhibitor is bound deep within a narrow pocket formed by the inter lobe cleft of the PknG domain.The main chain Glu233:O and Val235:NH of PknG form hydrogen bonds with AX20017.AX20017 results in mycobacterial transfer to lysosomes and killing of the mycobacteria. AX20017 does not affect the human kinases, whereas the activity of PknG is effectively inhibited. AX20017 does not affect cellular morphology, membrane ruffling, or macropinocytosis.
体内研究	负荷BT474乳腺肿瘤异种移植物的小鼠，afuresertib (p.o.)以每天10，30或100 mg/kg的剂量给药，分别导致8，37和61% TGI。负荷SKOV3卵巢肿瘤异种移植物的小鼠用10，30和100 mg/kg afuresertib处理，分别导致23，37 和97% TGI。
特征

推荐实验方法(仅供参考)

激酶实验：

Kinase Assay

In vitro phosphorylation by PknG (0.5μg) is in 25mM Tris (pH 7.5), 2mM MnCl2, and 0.5μCi [γ-32P]ATP in the absence or presence of the reagents. To monitor kinase activity of PknGΔN, the protein is combined with equal amounts of the kinase dead mutant of full-length PknG, PknG-K181M. To analyze kinase activity of PknG-I87S/A92S and PknG-C/S,the PknG-Nterminal fragment of PknG (2μg) is included. Phosphorylated proteins are separated on 12.5% SDS/PAGE and analyzed by autoradiography or quantitated by PhosphorImage analysis. IC50 values are determined by using a radiometric ATP consumptive assay. Twelve concentrations of AX20017 in the range from 5 × 10-5M to 1.5 × 10-10 M are tested in each kinase assay.

细胞实验:

Cell Assay

Phagocytosis is analyzed after incubation of J774 cells for 30 min in the presence of the indicated concentration of AX20017(0, 10, 20μM), followed by incubating the cells for 2 h with latex beads at a ratio of 10:1 beads/cells in the continued presence of the inhibitor, followed by fixation in 3% paraformaldehyde as described. Cells are observed with a Axiophot using a ×63 objective. Proliferation of J774 cells is analyzed by incorporation of tritiated thymidine (0.1μCi) for 12 h as described of cells that had been incubated for 48 h in the absence or presence of the AX20017(0, 10, 20μM).

保存条件：

-20℃

UN码：

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