140651-18-9
140651-18-9 結(jié)構(gòu)式
基本信息
CAY10574
CAN-508 (CAN508)
Cdk9 Inhibitor II
4-[2-(3,5-diamino-1H-pyrazol-4-yl)diazen-1-yl]phenol
CaMKII Inhibitor, CK59 - CAS 140651-18-9 - Calbiochem
物理化學(xué)性質(zhì)
常見問題列表
|
CDK9/cyclinT1 0.35 μM (IC 50 ) |
CDK2/cyclinE 20 μM (IC 50 ) |
cdk2/cyclin A 69 μM (IC 50 ) |
Cdk4/cyclin D1 13.5 μM (IC 50 ) |
CDK7/cyclin H 26 μM (IC 50 ) |
Cdk1/cyclin B 44 μM (IC 50 ) |
CAN508 reduces the frequency of S-phase cells of the cancer cell line HT-29 in antiproliferation assays.
CAN508 (20-40 μM; 72 hours) significantly reduces cell proliferation in a dose dependent manner in all three esophageal adenocarcinoma cell lines (SKGT4, OE33 and FLO-1 cells) with IC
50
s ranging from 34.99 to 91.09 μM.
CAN508 (40 μM; 72 hours) increases apoptosis in all three esophageal adenocarcinoma cells.
Apoptosis Analysis
| Cell Line: | SKGT4, OE33 and FLO-1 cells |
| Concentration: | 40 μM |
| Incubation Time: | 72 hours |
| Result: | Increased apoptosis by 2 fold in all three esophageal adenocarcinoma cells compared to untreated controls. |
CAN508 (60 mg/kg; i.p.; daily for 10 days) has antitumor effects in esophageal adenocarcinoma xenografts.
| Animal Model: | 4 weeks-old female nude mice (esophageal adenocarcinoma xenografts) |
| Dosage: | 60 mg/kg |
| Administration: | I.p.; daily for 10 days |
| Result: | Caused reduction of tumor growth starting from post-treatment day three with 50.83% reduction. |