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FIT-039

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Catalog No. T8972Cas No. 1113044-49-7

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.

FIT-039

FIT-039

🥰Excellent
Purity: 98.61%
Catalog No. T8972Cas No. 1113044-49-7
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 SizePriceAvailabilityQuantity
5 mg$31In Stock
10 mg$50In Stock
25 mg$103In Stock
50 mg$167In Stock
100 mg$251In Stock
200 mg$372In Stock
1 mL x 10 mM (in DMSO)$34In Stock
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Purity:98.61%
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Product Introduction

Bioactivity
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]
Chemical Properties
Molecular Weight315.41
FormulaC17H18FN3S
Cas No.1113044-49-7
SmilesFc1ccc(N2CCCCC2)c(NC(=S)c2ccncc2)c1
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM3.1705 mL15.8524 mL31.7048 mL158.5238 mL
5 mM0.6341 mL3.1705 mL6.3410 mL31.7048 mL
10 mM0.3170 mL1.5852 mL3.1705 mL15.8524 mL
20 mM0.1585 mL0.7926 mL1.5852 mL7.9262 mL
50 mM0.0634 mL0.3170 mL0.6341 mL3.1705 mL

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