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.

Product information

CAS Number: 1604810-84-5

Molecular Weight: 566.05

Formula: C31H28ClN7O2

Chemical Name: N-(3-{[5-chloro-4-(1H-indol-3-yl)pyrimidin-2-yl]amino}phenyl)-3-[4-(dimethylamino)but-2-enamido]benzamide

Smiles: CN(C)CC=CC(=O)NC1C=C(C=CC=1)C(=O)NC1C=C(C=CC=1)NC1N=C(C(Cl)=CN=1)C1=CNC2=CC=CC=C21

InChiKey: FONRCZUZCHXWBD-VGOFMYFVSA-N

InChi: 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+

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Solubility (25°C). 100 mg/mL(176.66 mM). ˂1 mg/mL.

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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.

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.

Products are for research use only. Not for human use.