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THZ2 CDK inhibitor

Cat.No.S7969

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

Chemical Structure

Molecular Weight: 566.05

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S796901 DMSO]100 mg/mL]false]Water]˂1 mg/mL]false]Ethanol]˂1 mg/mL]false Purity: 99.65%
99.65

Chemical Information, Storage & Stability

Molecular Weight 566.05 Formula

C31H28ClN7O2

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1604810-84-5 -- Storage of Stock Solutions

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

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (176.66 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : ˂1 mg/mL

Ethanol : ˂1 mg/mL

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Mechanism of Action

Targets/IC50/Ki
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. This compound 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 this compound is markedly reduced as compared to that of control tumors, demonstrating an anti-tumor activity of this chemical. Both acute and chronic exposure to it 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 this agent has reduced proliferation and increased apoptosis. It is able to efficiently reduce tumor cell proliferation and induce cell death in vivo.[1]
References

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