2136270-20-5
中文名稱
SPOP-IN-6b
英文名稱
SPOP-IN-6b
CAS
2136270-20-5
分子式
C28H32N6O3
分子量
500.59
MOL 文件
2136270-20-5.mol
更新日期
2024/11/12 15:28:26
2136270-20-5 結(jié)構(gòu)式
基本信息
中文別名
化合物 T16922化合物SPOP-IN-6B
英文別名
SPOP-IN-6b2H-Dipyrido[1,2-a:2',3'-d]pyrimidine-3-carboxamide, 1,5-dihydro-2-imino-10-methyl-N-[3-(4-morpholinyl)propyl]-5-oxo-1-(2-phenylethyl)-
物理化學(xué)性質(zhì)
密度1.32±0.1 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度DMSO: 10 mg/mL (19.98 mM)
酸度系數(shù)(pKa)11.90±0.20(Predicted)
形態(tài)Solid
顏色Light yellow to yellow
常見問題列表
生物活性
SPOP-IN-6b 是一種 SPOP 抑制劑,來自專利 CN 107141287,化合物 SPOP-B-88。靶點
SPOP
體外研究
SPOP-IN-6b a SPOP inhibitor with an IC
50
of 3.58 μM in cell assay.
SPOP-IN-6b (0.1-3.0 μM; 10 hours) can suppress SPOP activity, and then increase suppression cancer substrate protein PTEN and DUSP7 content.
SPOP-IN-6b suppresses intracellular SPOP acted on substrate PTEN ubiquitination.
Cell Viability Assay
Cell Line: | A498 cells |
Concentration: | 0.1 μM, 0.3 μM, 1.0 μM, 3.0 μM |
Incubation Time: | 10 hours |
Result: | Suppress SPOP activity, and then increase suppression cancer substrate protein PTEN and DUSP7 content. |
體內(nèi)研究
SPOP-IN-6b (40-80 mg/kg; i.p.; daily; for 25 days) can slow down the growth of tumour by suppressing SPOP.
Animal Model: | Nude mice |
Dosage: | 40 mg/kg, 60 mg/kg, 80 mg/kg |
Administration: | Intraperitoneal injection; daily; for 25 days |
Result: | Slowed down the growth of tumour by suppressing SPOP. |