FIT-039

SKU: orb1298481

Description

FIT-039 is an orally bioavailable, ATP-competitive CDK9 inhibitor with antiviral activity. It potently suppresses the replication of multiple DNA viruses, including HSV-1, HSV-2, adenovirus, and CMV, and shows promise for research against drug-resistant viral strains in both cellular and animal models.

Research Area

Cell Biology, Infectious Disease & Virology, Molecular Biology

Key Properties

• CAS Number: 1113044-49-7
• MW: 315.41
• Purity: 98.61% (May vary between batches)
• Formula: C₁₇H₁₈FN₃S
• SMILES: Fc1ccc(N2CCCCC2)c(NC(=S)c2ccncc2)c1
• Target: CDK,Virus Protease,HSV,DNA/RNA Synthesis
• Solubility: 10% DMSO+90% Corn Oil:2 mg/mL (6.34 mM);DMSO:30 mg/mL (95.11 mM)

Bioactivity

• Target IC50:
  CDK9-CyclinT1:5.8 μM|HSV1:0.69 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.
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• 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
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Herpes simplex virus, FIT 039, FIT039, FIT-039, HSV-2, HSV-1, HSV, Inhibitor, inhibit, mRNA, orally, antiviral, CDK9, CDK9/cyclin T1, CDK, CMV, Cytomegalovirus, Cyclin dependent kinase, DNASynthesis, DNA, DNA Synthesis, DNA/RNA Synthesis, polymerase-II, RNASynthesis, RNA Synthesis, transcription, viruses

Compound Identifiers

PubChem CID

25186688