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FIT-039

Catalog No. T8972 CAS 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.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

FIT-039, CAS 1113044-49-7

Pack Size	Availability	Price/USD
5 mg	In stock	$ 51.00
10 mg	In stock	$ 84.00
25 mg	In stock	$ 172.00
50 mg	In stock	$ 278.00
100 mg	In stock	$ 418.00
500 mg	In stock	$ 988.00
1 mL * 10 mM (in DMSO)	In stock	$ 57.00

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Purity: 100%

Biological Description

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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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 30 mg/mL (95.11 mM)

References and Literature

1. Ajiro M , Sakai H , Onogi H , et al. CDK9 Inhibitor FIT-039 Suppresses Viral Oncogenes E6 and E7 and Has a Therapeutic Effect on HPV-Induced Neoplasia.[J]. 2018.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Kinase Inhibitor Library Bioactive Compound Library Bioactive Compounds Library Max ReFRAME Related Library Anti-Infection Compound Library Anti-Pancreatic Cancer Compound Library Anti-Viral Compound Library Anti-Breast Cancer Compound Library Cell Cycle Compound Library

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Related compounds with same targets

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Keywords

FIT-039 1113044-49-7 Cell Cycle/Checkpoint DNA Damage/DNA Repair Microbiology/Virology Others DNA/RNA Synthesis CDK HSV Cytomegalovirus HSV-1 Herpes simplex virus transcription FIT 039 Inhibitor DNA Cyclin dependent kinase CDK9 CMV mRNA FIT039 viruses antiviral inhibit orally polymerase-II HSV-2 inhibitor

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