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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.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $31 | In Stock | |
10 mg | $50 | In Stock | |
25 mg | $103 | In Stock | |
50 mg | $167 | In Stock | |
100 mg | $251 | In Stock | |
200 mg | $372 | In Stock | |
1 mL x 10 mM (in DMSO) | $34 | In Stock |
Description | 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. |
Targets&IC50 | HSV1:0.69 μM, CDK9-CyclinT1:5.8 μM |
In vitro | 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]. |
Cell Research | 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] |
Molecular Weight | 315.41 |
Formula | C17H18FN3S |
Cas No. | 1113044-49-7 |
Smiles | Fc1ccc(N2CCCCC2)c(NC(=S)c2ccncc2)c1 |
Relative Density. | no data available |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 30 mg/mL (95.11 mM) | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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