A-366
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- CAS号:
- 1527503-11-2
- 英文名:
- 5'-Methoxy-6'-[3-(1-pyrrolidinyl)propoxy]spiro[cyclobutane-1,3'-[3H]indol]-2'-amine
- 英文别名:
- A-336;A-366;CS-2077;A-366,MV4;A-366; A366;A 366;5'-methoxy-6'-(3-(pyrrolidin-1-yl)propoxy)spiro[cyclobutane-1,3'-indol]-2'-amine;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;5'-Methoxy-6'-[3-(1-pyrrolidinyl)propoxy]spiro[cyclobutane-1,3'-[3H]indol]-2'-amine;Spiro[cyclobutane-1,3'-[3H]indol]-2'-amine, 5'-methoxy-6'-[3-(1-pyrrolidinyl)propoxy]-
- 中文名:
- A-366
- 中文别名:
- 化合物A366;G9A/GLP抑制剂(A-366);A 366,G9A / GLP抑制剂;5'-甲氧基-6'-(3-(吡咯烷-1-基)丙氧基)螺[环丁烷-1,3'-吲哚] -2'-胺;5'-甲氧基-6'-(3-(吡咯烷-1-基)丙氧基)螺[环丁烷-1,3'-吲哚] -2'-胺
- CBNumber:
- CB43038523
- 分子式:
- C19H27N3O2
- 分子量:
- 329.44
- MOL File:
- 1527503-11-2.mol
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A-366化学性质
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沸点:
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533.6±60.0 °C(Predicted)
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密度:
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1.29±0.1 g/cm3(Predicted)
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储存条件:
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2-8°C
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溶解度:
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DMSO : 50 mg/mL (151.77 mM; Need ultrasonic)
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酸度系数(pKa):
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10.18±0.20(Predicted)
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形态:
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powder
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颜色:
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white to beige
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A-366性质、用途与生产工艺
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。
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
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Cell Line:
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MV4;11 cells
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Concentration:
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0.01-10 μM
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Incubation Time:
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14 days
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Result:
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Resulted in inhibited proliferation and a decrease in viability corresponding to the dose response observed for CD11b staining.
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A-366 (30 mg/kg; osmotic mini-pump; daily for 14 days) treatment of MV4;11 xenografts elicits growth inhibition.
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Animal Model:
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6-8 week old SCID-beige female mice (MV4;11 xenografts)
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Dosage:
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30 mg/kg
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Administration:
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By osmotic mini-pump; daily for 14 days
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Result:
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A modest 45% tumor growth inhibition resulting from A-366 treatment in this model.
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A-366
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/01/25 | HY-12583 | A-366 | | 1 mg | 327元 |
| 2024/01/25 | HY-12583 | A-366
A-366 | 1527503-11-2 | 5mg | 750元 |
1527503-11-2, A-366 相关搜索:
- 合成有机化合物配体
- 细胞生物学试剂
- 抑制剂
- 5'-甲氧基-6'-(3-(吡咯烷-1-基)丙氧基)螺[环丁烷-1,3'-吲哚] -2'-胺
- A 366,G9A / GLP抑制剂
- 5'-甲氧基-6'-(3-(吡咯烷-1-基)丙氧基)螺[环丁烷-1,3'-吲哚] -2'-胺
- 化合物A366
- G9A/GLP抑制剂(A-366)
- 1527503-11-2
- 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,MV4
- 11,selective,cells,peptide-competitive,epigenetics,Inhibitor,interaction,inhibit,H3K4me3,Epigenetic Reader Domain,leukemia,Histone Methyltransferase,methyltransferase
- Spiro[cyclobutane-1,3'-[3H]indol]-2'-amine, 5'-methoxy-6'-[3-(1-pyrrolidinyl)propoxy]-
- 5'-methoxy-6'-(3-(pyrrolidin-1-yl)propoxy)spiro[cyclobutane-1,3'-indol]-2'-amine
- A-366; A366;A 366
- CS-2077
- A-336
- A-366
- 5'-Methoxy-6'-[3-(1-pyrrolidinyl)propoxy]spiro[cyclobutane-1,3'-[3H]indol]-2'-amine