A Cdk inhibitor
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AT7519 (hydrochloride)

Item No. 16231

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[(2,6-dichlorobenzoyl)amino]-N-4-piperidinyl-1H-pyrazole-3-carboxamide, monohydrochloride
CAS Number
902135-91-5
Molecular Formula
C16H17Cl2N5O2 • HCl
Formula Weight
418.7
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 25 mg/mlEthanol: 5 mg/mlPBS (pH 7.2): 0.5 mg/ml
λmax
268 nm
SMILES
O=C(NC1CCNCC1)C2=NNC=C2NC(C3=C(Cl)C=CC=C3Cl)=O.Cl
InChi Code
InChI=1S/C16H17Cl2N5O2.ClH/c17-10-2-1-3-11(18)13(10)15(24)22-12-8-20-23-14(12)16(25)21-9-4-6-19-7-5-9;/h1-3,8-9,19H,4-7H2,(H,20,23)(H,21,25)(H,22,24);1H
InChi Key
PAOFPNGYBWGKCO-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

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    10 mg

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    25 mg

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    Product Description

    AT7519 is an ATP-competitive inhibitor of cyclin-dependent kinases (Cdks) with IC50 values of 210, 47, 100, 13, 170, and <10 nM for Cdk1, 2, 4, 5, 6, and 9, respectively.1 It is less potent against Cdk3 and Cdk7 and inactive against non-Cdk kinases save for GSK3β (IC50 = 89 nM).1 AT7519 demonstrates antiproliferative activity against a wide variety of human tumor cell lines (IC50s = 40-940 nM in vitro), inhibiting cell cycle progression and inducing apoptosis, and prevents tumor growth in human tumor xenograft models.1,2 AT7519 induces activation of GSK3β by down-regulating GSK3β phosphorylation, which contributes to AT7519-induced apoptosis.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Squires, M.S., Feltell, R.E., Wallis, N.G., et al. Biological characterization of AT7519, a small-molecule inhibitor of cyclin-dependent kinases, in human tumor cell lines. Mol. Cancer Ther. 8(2), 324-332 (2009).

    2. Santo, L., Vallet, S., Hideshima, T., et al. AT7519, a novel small molecule multi-cyclin-dependent kinase inhibitor, induces apoptosis in multiple myeloma via GSK-βactivation and RNA polymerase II inhibition. Oncogene 29(16), 2325-2336 (2010).