CAN-508

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

CAN-508 是一种有效的选择性 CDK9 抑制剂，IC50 为 0.35 uM (CDK9/cyclin T1)，选择性是 CDK1/2/4/7 的 35 倍以上 (IC50=13.5-70 uM)。

CAN-508 is a potent, selective CDK9 inhibitor with IC50 of 0.35 uM (CDK9/cyclin T1), displays >35 fold selectivity over CDK1/2/4/7 (IC50=13.5-70 uM); reduces the frequency of S-phase cells of the cancer cell line HT-29 in antiproliferation assays; decreases phosphorylation of the retinoblastoma protein and the C-terminal domain of RNA polymerase II, inhibits mRNA synthesis, and induces the tumor suppressor protein p53.

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 IC50s 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.

CAN508

Angiogenesis

CDK

CDK

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140651-18-9

218.22

C9H10N6O

>98% (HPLC)

In Vitro:?DMSO : 250 mg/mL (1145.63 mM)

OC1=CC=C(/N=N/C2=C(N)NN=C2N)C=C1

4-[(3,5-diamino-1H-pyrazol-4-yl)azo]-phenol

(-20℃)

With Ice Pack

≥ 2 years