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FIT-039

Cat. No. M10707
FIT-039  Structure
Size Price Availability Quantity
5mg USD 82  USD82 In stock
10mg USD 131  USD131 In stock
25mg USD 260  USD260 In stock
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Quality Control & Documentation
Biological Activity

FIT-039 is a selective, ATP-competitive, orally active CDK9 inhibitor against CKD9/cyclin T1 IC50 Is 5.8 μM. FIT-039 does not inhibit other CDKs and other kinases. FIT-039 inhibits HSV-1 (IC50 is 0.69 μM), HSV-2, human adenovirus, and human CMV replication. FIT-039 is a promising antiviral agent that can be used to suppress resistant HSV and other DNA viruses.

Chemical Information
Molecular Weight 315.41
Formula C17H18FN3S
CAS Number 1113044-49-7
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Phattharachanok Khumkhrong, et al. Biomolecules. Crinamine Induces Apoptosis and Inhibits Proliferation, Migration, and Angiogenesis in Cervical Cancer SiHa Cells

[2] Masahiko Ajiro, et al. Clin Cancer Res. CDK9 Inhibitor FIT-039 Suppresses Viral Oncogenes E6 and E7 and Has a Therapeutic Effect on HPV-Induced Neoplasia

[3] Tomohisa Tanaka, et al. Antiviral Res. Inhibitory effect of CDK9 inhibitor FIT-039 on hepatitis B virus propagation

[4] Mika Okamoto, et al. Antiviral Res. Selective inhibition of HIV-1 replication by the CDK9 inhibitor FIT-039

[5] Makoto Yamamoto, et al. J Clin Invest. CDK9 inhibitor FIT-039 prevents replication of multiple DNA viruses

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  Catalog
Abmole Inhibitor Catalog




Keywords: FIT-039 supplier, CDK, inhibitors, activators


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