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
生物活性体外研究体内研究 用途与合成方法 MSDS 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)-二酮价格(试剂级) 上下游产品信息
| 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 |
|---|---|
| 中文同义词 | 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;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 |
| 英文同义词 | GSK621;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)-;GSK621 >=98% (HPLC);GSK621 (GSK 621;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;Apoptosis,CHOP,GSK 621,inhibit,AMP-activated protein kinase,Inhibitor,UPR,PERK,GSK621,Autophagy,GSK-621,ATF4,AMPK,ER Stress;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 |
| CAS号 | 1346607-05-3 |
| 分子式 | C26H20ClN3O5 |
| 分子量 | 489.91 |
| EINECS号 | |
| 相关类别 | 抑制剂 |
| Mol文件 | 1346607-05-3.mol |
| 结构式 | ![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 结构式](CAS/20200611/GIF/1346607-05-3.gif) |
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 性质
| 密度 | 1.41±0.1 g/cm3(Predicted) |
|---|---|
| 储存条件 | 2-8°C |
| 溶解度 | 不溶于水；不溶于乙醇； DMSO 中≥28.5 mg/mL |
| 形态 | 结晶固体 |
| 酸度系数(pKa) | 9.01±0.40(Predicted) |
| 颜色 | 米白色至浅黄色 |
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)。
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. |
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. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-100548 | GSK621 | 1 mg | 514元 | |
| 2024/04/30 | HY-100548 | 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 GSK621 | 1346607-05-3 | 5mg | 1350元 |