A covalent Cdk7 inhibitor
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Isomer(s)
31055THZ2
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THZ1

Item No. 9002215

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[3-[[5-chloro-4-(1H-indol-3-yl)-2-pyrimidinyl]amino]phenyl]-4-[[(2E)-4-(dimethylamino)-1-oxo-2-buten-1-yl]amino]-benzamide
CAS Number
1604810-83-4
Molecular Formula
C31H28ClN7O2
Formula Weight
566.1
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMF:PBS (pH 7.2) (1:2): 0.3 mg/mlDMSO: 25 mg/ml
λmax
214, 295 nm
SMILES
CN(C/C=C/C(NC1=CC=C(C(NC2=CC(NC3=NC=C(Cl)C(C4=CNC5=C4C=CC=C5)=N3)=CC=C2)=O)C=C1)=O)C
InChi Code
InChI=1S/C31H28ClN7O2/c1-39(2)16-6-11-28(40)35-21-14-12-20(13-15-21)30(41)36-22-7-5-8-23(17-22)37-31-34-19-26(32)29(38-31)25-18-33-27-10-4-3-9-24(25)27/h3-15,17-19,33H,16H2,1-2H3,(H,35,40)(H,36,41)(H,34,37,38)/b11-6+
InChi Key
OBJNFLYHUXWUPF-IZZDOVSWSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

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    Product Description

    THZ1 is a Cdk7 inhibitor (IC50s = 3.2-15.6 nM in vitro) that selectively targets a remote cysteine residue located outside of the classic kinase domain.1 THZ1 also targets Cdk12 kinase activity although at a higher concentration (IC50 = 250 nM).1 It displays broad anti-proliferative activity against cancer cell lines, particularly T-ALL cell lines that display characteristic misregulation of T cell lineage-specific transcription factors.1 THZ1 is reported to induce apoptotic cell death in triple-negative breast cancer cells that are highly dependent on Cdk7.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Kwiatkowski, N., Zhang, T., Rahl, P.B., et al. Targeting transcription regulation in cancer with a covalent CDK7 inhibitor. Nature 511(7511), 616-620 (2014).

    2. Wang, Y., Zhang, T., Kwiatkowski, N., et al. CDK7-dependent transcriptional addiction in triple-negative breast cancer. Cell 163(1), 174-186 (2015).