A Cdk7 inhibitor
Related Products
Isomer(s)
9002215THZ1
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THZ2

Item No. 31055

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]-3-[[(2E)-4-(dimethylamino)-1-oxo-2-buten-1-yl]amino]-benzamide
CAS Number
1604810-84-5
Molecular Formula
C31H28ClN7O2
Formula Weight
566.1
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:2): 0.3 mg/ml
λmax
214, 278 nm
SMILES
CN(C)C/C=C/C(NC1=CC(C(NC2=CC(NC3=NC(C4=CNC5=CC=CC=C54)=C(Cl)C=N3)=CC=C2)=O)=CC=C1)=O
InChi Code
InChI=1S/C31H28ClN7O2/c1-39(2)15-7-14-28(40)35-21-9-5-8-20(16-21)30(41)36-22-10-6-11-23(17-22)37-31-34-19-26(32)29(38-31)25-18-33-27-13-4-3-12-24(25)27/h3-14,16-19,33H,15H2,1-2H3,(H,35,40)(H,36,41)(H,34,37,38)/b14-7+
InChi Key
FONRCZUZCHXWBD-VGOFMYFVSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    10 mg

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    Product Description

    THZ2 is a Cdk7 inhibitor (IC50 = 13.9 nM) and a derivative of THZ1 (Item No. 9002215).1 It is selective for Cdk7 over Cdk1, -2, -5, -8, and -9 (IC50s = 96.9, 222, 134, 6,830, and 194 nM, respectively). THZ2 (0.001-1 nM) reduces proliferation of BT-549, HCC70, and MDA-MB-468 triple-negative breast cancer (TNBC) cells. In vivo, THZ2 (10 mg/kg) reduces tumor volume in an MDA-MB-231 mouse xenograft model. It also reduces tumor weight and volume, as well as the number of lung metastases, in an SJSA-1 osteosarcoma orthotopic mouse xenograft model.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

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

    2. Zhang, J., Liu, W., Zou, C., et al. Targeting super-enhancer-associated oncogenes in osteosarcoma with THZ2, a vovalent CDK7 inhibitor. Clin. Cancer Res. 26(11), 2681-2692 (2020).