| 名称 | FIT-039 |
| 描述 | FIT-039 is a selective and ATP-competitive, orally active inhibitor of CDK9( IC50 : 5.8 μM;CDK9/cyclin T1). FIT-039 inhibits replication of HSV-1 (IC50 of 0.69 μM), HSV-2, human adenovirus, and human CMV. FIT-039 is a promising antiviral agent for inhibiting drug-resistant HSVs and other DNA viruses. |
| 细胞实验 | Examined FIT-039 for its effect on HPV gene expression in HPV+ cervical cancer cells.?Primary keratinocytes monolayer and organotypic raft culture models were used to evaluate HPV viral replication and cervical intraepithelial neoplasia (CIN) phenotypes.?Preclinical pharmacokinetics and toxicity tests for FIT-039 were also conducted.?Finally, the anti-HPV effect of FIT-039 was further examined in vivo, using HPV+ cervical cancer xenografts[1] |
| 体外活性 | FIT-039 inhibits HPV replication and expression of E6 and E7 viral oncogenes, restoring tumor suppressors p53 and pRb in HPV+?cervical cancer cells. The therapeutic effect of FIT-039 was demonstrated in CIN model of an organotypic raft culture, where FIT-039 suppressed HPV18-induced dysplasia/hyperproliferation with reduction in viral load. FIT-039 also repressed growth of HPV16+, but not HPV-?cervical cancer xenografts without any significant adverse effects. Safety and pharmacokinetics of FIT-039 were confirmed for systemic and topical routes[1]. |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 30 mg/mL (95.11 mM)
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| 关键字 | Cytomegalovirus | HSV-1 | Herpes simplex virus | transcription | FIT 039 | Inhibitor | DNA | CDK | Cyclin dependent kinase | CDK9 | CMV | mRNA | FIT-039 | FIT039 | viruses | antiviral | inhibit | orally | polymerase-II | HSV-2 | DNA/RNA Synthesis | HSV |
| 相关产品 | Rifampicin | 5-Fluorouracil | Ribavirin | Guanidine hydrochloride | 2,4-D | Resveratrol | 2-Deoxy-D-glucose | Oxyresveratrol | Acyclovir | Thymidine | Temozolomide | Folic acid |
| 相关库 | 抗胰腺癌化合物库 | 经典已知活性库 | 激酶抑制剂库 | 抗病毒库 | 抑制剂库 | NO PAINS 化合物库 | 口服活性化合物库 | 抗衰老化合物库 | 已知活性化合物库 | 抗癌化合物库 |
United States
