A-366

生物活性体外研究体内研究 A-366 试剂级价格

A-366

CAS号:1527503-11-2
英文名:5'-Methoxy-6'-[3-(1-pyrrolidinyl)propoxy]spiro[cyclobutane-1,3'-[3H]indol]-2'-amine
中文名:A-366
CBNumber:CB43038523
分子式:C19H27N3O2
分子量:329.44
MOL File:1527503-11-2.mol

A-366化学性质

沸点 :533.6±60.0 °C(Predicted)
密度 :1.29±0.1 g/cm3(Predicted)
储存条件 :2-8°C
溶解度 :DMSO : 50 mg/mL (151.77 mM; Need ultrasonic)
酸度系数(pKa) :10.18±0.20(Predicted)
形态 :powder
颜色 :white to beige

安全信息

危险品运输编号 :UN 3077 9 / PGIII
WGK Germany :3

A-366性质、用途与生产工艺

生物活性 A-366 是一种高效、高选择性的肽竞争性组蛋白甲基转移酶 G9a 抑制剂，对 G9a 和 GLP 的 IC50 分别为 3.3 和 38 nM。A-366 比其他 21 种甲基转移酶具有 1000 倍以上的选择性。A-366 是一种有效的 Spindlin1-H3K4me3 相互作用的抑制剂 (IC50=182.6 nM)。A-366 对人 H3R (Ki=17 nM) 表现出很高的亲和力，并且在组胺能和多巴胺能受体家族的亚群间表现出亚型选择性。

体外研究

A-366 (0.01-10 μM; 14 days) induces differentiation and affects viability in MV4;11 cells.
A-366 (0.3-3 μM; 72 hours) reduces the total levels of H3K9me2 in a time and concentration dependent manner with a cellular EC50 of ~300 nM in PC-3 prostate adenocarcinoma cells. A-366 (0.01-10 μM; 4 days; HL-60 cells) results in a dose-dependent differentiation and a corresponding decrease in proliferation. DNA content analysis of A-366-treated HL-60 cells showed an accumulation of cells in G1 consistent with cytostasis.

Cell Viability Assay

Cell Line:	MV4;11 cells
Concentration:	0.01-10 μM
Incubation Time:	14 days
Result:	Resulted in inhibited proliferation and a decrease in viability corresponding to the dose response observed for CD11b staining.

体内研究

A-366 (30 mg/kg; osmotic mini-pump; daily for 14 days) treatment of MV4;11 xenografts elicits growth inhibition.

Animal Model:	6-8 week old SCID-beige female mice (MV4;11 xenografts)
Dosage:	30 mg/kg
Administration:	By osmotic mini-pump; daily for 14 days
Result:	A modest 45% tumor growth inhibition resulting from A-366 treatment in this model.