A CDK7 inhibitor
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LDC-4297

Item No. 23398

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
8-(1-methylethyl)-2-(3-piperidinyloxy)-N-[[2-(1H-pyrazol-1-yl)phenyl]methyl]-pyrazolo[1,5-a]-1,3,5-triazin-4-amine
CAS Number
1453834-21-3
Molecular Formula
C23H28N8O
Formula Weight
432.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 20 mg/mlEthanol: 20 mg/ml
SMILES
CC(C)C(C=N1)=C(N1C(NCC2=CC=CC=C2N3C=CC=N3)=N4)N=C4OC5CNCCC5
InChi Code
InChI=1S/C23H28N8O/c1-16(2)19-15-27-31-21(19)28-23(32-18-8-5-10-24-14-18)29-22(31)25-13-17-7-3-4-9-20(17)30-12-6-11-26-30/h3-4,6-7,9,11-12,15-16,18,24H,5,8,10,13-14H2,1-2H3,(H,25,28,29)
InChi Key
LSGRZENCFIIHNV-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    LDC-4297 is an inhibitor of cyclin-dependent kinase 7 (CDK7; IC50 = <5 nM).1 It is selective for CDK7 over CDK4, CDK6, and CDK9 (IC50s = >10, >10, and 1.71 μM), however, it also inhibits CDK2 and CDK1 (IC50s = 6.4 and 53.7 nM, respectively). LDC-4297 (10-100 nM) induces apoptosis in A549, HeLa, and HCT116 cancer cells in a concentration-dependent manner. It inhibits human cytomegalovirus (HCMV) replication in human fibroblasts (EC50 = 24.5 nM).2 LDC-4297 also reduces replication of Herpesviridae, Adenoviridae, Poxviridae, Retroviridae, and Orthomyxoviridae family viruses (EC50s = 0.02-1.13 μM).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Kelso, T.W.R., Baumgart, K., Eickhoff, J., et al. Cyclin-dependent kinase 7 controls mRNA synthesis by affecting stability of preinitiation complexes, leading to altered gene expression, cell cycle progression, and survival of tumor cells. Mol. Cell. Biol. 34(19), 3675-3688 (2014).

    2. Hutterer, C., Eickhoff, J., Milbradt, J., et al. A novel CDK7 inhibitor of the pyrazolotriazine class exerts broad-spectrum antiviral activity at nanomolar concentrations. Antimicrob. Agents Chemother. 59(4), 2062-2071 (2015).