1527503-11-2
中文名稱
A-366
英文名稱
5'-Methoxy-6'-[3-(1-pyrrolidinyl)propoxy]spiro[cyclobutane-1,3'-[3H]indol]-2'-amine
CAS
1527503-11-2
分子式
C19H27N3O2
分子量
329.44
MOL 文件
1527503-11-2.mol
更新日期
2024/07/01 17:51:34
1527503-11-2 結(jié)構(gòu)式
基本信息
中文別名
化合物A366G9A/GLP抑制劑(A-366)
英文別名
A-336A-366
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
Spiro[cyclobutane-1,3'-[3H]indol]-2'-amine, 5'-methoxy-6'-[3-(1-pyrrolidinyl)propoxy]-
所屬類別
生物化工：激動(dòng)劑抑制劑物理化學(xué)性質(zhì)
沸點(diǎn)533.6±60.0 °C(Predicted)
密度1.29±0.1 g/cm3(Predicted)
儲(chǔ)存條件2-8°C
溶解度DMSO : 50 mg/mL (151.77 mM; Need ultrasonic)
酸度系數(shù)(pKa)10.18±0.20(Predicted)
形態(tài)粉末
顏色白色至米色
常見問題列表
生物活性
A-366 是一種高效、高選擇性的肽競爭性組蛋白甲基轉(zhuǎn)移酶 G9a 抑制劑，對(duì) G9a 和 GLP 的 IC50 分別為 3.3 和 38 nM。A-366 比其他 21 種甲基轉(zhuǎn)移酶具有 1000 倍以上的選擇性。A-366 是一種有效的 Spindlin1-H3K4me3 相互作用的抑制劑 (IC50=182.6 nM)。A-366 對(duì)人 H3R (Ki=17 nM) 表現(xiàn)出很高的親和力，并且在組胺能和多巴胺能受體家族的亞群間表現(xiàn)出亞型選擇性。體外研究
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. |
體內(nèi)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. |