A-366
中文名称:
A-366
中文同义词:
G9A/GLP抑制剂(A-366);化合物A366
英文名称:
5-Methoxy-6-[3-(1-pyrrolidinyl)propoxy]spiro[cyclobutane-1,3-[3H]indol]-2-amine
英文同义词:
CS-2077;A-366; A366;A 366;5-methoxy-6-(3-(pyrrolidin-1-yl)propoxy)spiro[cyclobutane-1,3-indol]-2-amine;5-Methoxy-6-[3-(1-pyrrolidinyl)propoxy]spiro[cyclobutane-1,3-[3H]indol]-2-amine;A-366;A-336;Spiro[cyclobutane-1,3-[3H]indol]-2-amine, 5-methoxy-6-[3-(1-pyrrolidinyl)propoxy]-
CAS号:
1527503-11-2
分子式:
C19H27N3O2
分子量:
329.44
EINECS号:
808-907-0
相关类别:
细胞生物学试剂;抑制剂
Mol文件:
1527503-11-2.mol
沸点
533.6±60.0 °C(Predicted)
密度
1.29±0.1 g/cm3(Predicted)
储存条件
2-8°C
形态
powder
酸度系数(pKa)
10.18±0.20(Predicted)
颜色
white to beige
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.
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.
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.
危险品运输编号
UN 3077 9 / PGIII
WGK Germany
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