1346607-05-3
中文名称
6-氯-5-(2'-羟基-3'-甲氧基-[1,1'-联苯]-4-基)-3-(3-甲氧基苯基)-1H-吡咯并[3,2-D]嘧啶-2,4(3H,5H)-二酮
英文名称
GSK621
CAS
1346607-05-3
分子式
C26H20ClN3O5
分子量
489.91
MOL 文件
1346607-05-3.mol
更新日期
2023/11/28 16:55:52
1346607-05-3 结构式
基本信息
中文别名
6-氯-5-(2'-羟基-3'-甲氧基-[1,1'-联苯]-4-基)-3-(3-甲氧基苯基)-1H-吡咯并[3,2-D]嘧啶-2,4(3H,5H)-二酮 英文别名
GSK621GSK621 (GSK 621
GSK621 >=98% (HPLC)
6-Chloro-5-(2'-hydroxy-3'-methoxy-[1,1'-biphenyl]-4-yl)-3-(3-methoxyphenyl)-1H-pyrrolo[3,2-d]pyrimidine-2,4(3H,5H)-dione
1H-Pyrrolo[3,2-d]pyrimidine-2,4(3H,5H)-dione, 6-chloro-5-(2'-hydroxy-3'-methoxy[1,1'-biphenyl]-4-yl)-3-(3-methoxyphenyl)-
所属类别
医药中间体：杂环化合物物理化学性质
密度1.41±0.1 g/cm3(Predicted)
储存条件Sealed in dry,2-8°C
溶解度insoluble in H2O; insoluble in EtOH; ≥28.5 mg/mL in DMSO
酸度系数(pKa)9.01±0.40(Predicted)
形态结晶固体
颜色Off-white to light yellow
常见问题列表
生物活性
GSK621 是特异性的 AMPK 激动剂，其对 AML 细胞系的IC50 值为13-30 μM。GSK621 可诱导自噬和凋亡。GSK621 可诱导eiF2α 磷酸化 (UPR 激活的一个标志)。体外研究
GSK621 (30 μM) induces AMPKα T172, ACC (S79) and ULK1 (S555) phosphorylation.
GSK621 (30 μM) induces autophagy and apoptosis.
GSK621 treatment also induces PERK phosphorylation, a marker of ER stress, in AML cells.
Cell Proliferation Assay
| Cell Line: | MV4-11, OCI-AML3, OCI-AML2, HL-60, Kasumi, HEL, UT7, NB4, TF-1, KG1A, Nomo p28, SKM-1, U937, YHP1, MOLM-14, Mo7e, K562, MOLM-13, EOL-1, SET-2 AML cell lines. 0-30 μM. |
| Concentration: | 0-30 μM. |
| Incubation Time: | 4 d. |
| Result: |
IC
50
values ranged from 13 to 30 μM.
Reduced the proliferation of all 20 lines and increased apoptosis in 17 (85%) lines. |
Cell Autophagy Assay.
| Cell Line: | AML cell lines and primary AML samples. |
| Concentration: | 30 μM. |
| Incubation Time: | 24 h. |
| Result: | Induced the formation of numerous intracytoplasmic vacuoles including autophagosomes. |
体内研究
GSK621 (30 mg/kg, ip twice daily) exhibits significant anti-tumor activity in MOLM-14 cells xenograft.
| Animal Model: | MOLM-14 cells xenografted into nude mice. |
| Dosage: | 30 mg/kg. |
| Administration: | IP twice daily. |
| Result: | Reduced leukemia growth and significantly extended survival compared to vehicle-treated animals or those treated with 10 mg/kg twice daily. |