A Cdk9 inhibitor
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FIT-039

Item No. 36555

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[5-fluoro-2-(1-piperidinyl)phenyl]-4-pyridinecarbothioamide
CAS Number
1113044-49-7
Molecular Formula
C17H18FN3S
Formula Weight
315.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: 10 mM
SMILES
FC1=CC=C(N2CCCCC2)C(NC(C3=CC=NC=C3)=S)=C1
InChi Code
InChI=1S/C17H18FN3S/c18-14-4-5-16(21-10-2-1-3-11-21)15(12-14)20-17(22)13-6-8-19-9-7-13/h4-9,12H,1-3,10-11H2,(H,20,22)
InChi Key
VRKZHYSJZOUICG-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $96

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    10 mg

    $174

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    25 mg

    $390

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    Product Description

    FIT-039 is an inhibitor of cyclin-dependent kinase 9 (Cdk9; IC50 = 5.8 µM for Cdk9/cyclin T1).1 It is selective for Cdk9/cyclin T1 over Cdk4/cyclin D3 at 30 µM and Cdk2/cyclin A2, Cdk2/cyclin E1, Cdk5/p25, Cdk6/cyclin D3, and Cdk7/cyclin/MAT1 at 10 µM but also inhibits GSK3α, GSK3β, PKN1, haspin, p70S6K, DYRK1B, DYRK3, and IRR at 10 µM. FIT-039 inhibits DNA replication of herpes simplex virus 1 (HSV-1) in HeLa cells (IC50 = 0.69 µM). Topical application of FIT-039 (1.25-10% w/w) reduces skin lesions and improves survival in HSV-1-infected mice. FIT-039 (300 mg/kg) also reduces tumor growth in a human papillomavirus (HPV) type 16-positive Ca Ski cervical cancer mouse xenograft model.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Yamamoto, M., Onogi, H., Kii, I., et al. CDK9 inhibitor FIT-039 prevents replication of multiple DNA viruses. J. Clin. Invest. 124(8), 3479-3488 (2014).

    2. 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. Clin. Cancer Res. 24(18), 4518-4528 (2018).