THZ2

For research use only.

Catalog No.S7969

THZ2 Chemical Structure

CAS No. 1604810-84-5

THZ2, a THZ1 analog, is a selective inhibitor of CDK7 with IC50 of 13.9 nM. THZ2 efficiently suppresses the clonogenic growth of TNBC cells with IC50 of ~10 nM.

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Biological Activity

Description THZ2, a THZ1 analog, is a selective inhibitor of CDK7 with IC50 of 13.9 nM. THZ2 efficiently suppresses the clonogenic growth of TNBC cells with IC50 of ~10 nM.
Targets
CDK7 [1]
(Cell-free assay)
13.9 nM
In vitro

THZ2 selectively targets CDK7 and potently inhibits the growth of triple-negative but not ER/PR+ breast cancer cells. THZ2 at low nanomolar doses also efficiently suppresses the clonogenic growth of TNBC cells.[1]

In vivo

THZ2 is well tolerated in nude mice. The growth rate of tumors in mice treated with THZ2 is markedly reduced as compared to that of control tumors, demonstrating an anti-tumor activity of THZ2. Both acute and chronic exposure to THZ2 significantly reduces CTD phosphorylation of RNAPII at all three phosphorylation sites (S2, S5, and S7), indicating that CDK7 is efficiently targeted in the tumor cells. Compared to vehicle-treated tumors, tumor tissues isolated from mice treated with THZ2 has reduced proliferation and increased apoptosis. THZ2 is able to efficiently reduce tumor cell proliferation and induce cell death in vivo.[1]

Protocol

Cell Research:

[1]

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  • Cell lines: BT549, CAMA1, HCC1187, HCC1569, HCC38, MDAMB-231, MDA-MB-415, MDA-MB-468, T47D, ZR-75-1, HEK293T cells
  • Concentrations: 200 nM, 500 nM
  • Incubation Time: 24 h, 48 h
  • Method:

    Cell Proliferation Assay: For 96-well plate assay, cells are plated at the density of 2000 cells per well, and on the next day treated with THZ2 of various concentrations. After 48-hour incubation, cells are fixed and stained with crystal violet. The staining is then extracted by adding each well with 10% acetic acid, with absorbance measured at 590 nm with 750 nm as a reference.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: Nude mice (Foxn1nu)
  • Dosages: 10 mg/kg
  • Administration: IP
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (176.66 mM)
Water ˂1 mg/mL
Ethanol ˂1 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 566.05
Formula

C31H28ClN7O2

CAS No. 1604810-84-5
Storage powder
in solvent
Synonyms N/A
Smiles CN(C)CC=CC(=O)NC1=CC=CC(=C1)C(=O)NC2=CC=CC(=C2)NC3=NC=C(C(=N3)C4=CNC5=CC=CC=C54)Cl

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID