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Chemical Structure| 1604810-83-4 Chemical Structure| 1604810-83-4

Structure of THZ1
CAS No.: 1604810-83-4

Chemical Structure| 1604810-83-4

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THZ1 is a selective and potent covalent CDK7 inhibitor with an IC50 of 3.2 nM. It also inhibits closely related kinases CDK12 and CDK13 and downregulates MYC expression.

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Product Details of THZ1

CAS No. :1604810-83-4
Formula : C31H28ClN7O2
M.W : 566.05
SMILES Code : O=C(NC1=CC=CC(NC2=NC=C(Cl)C(C3=CNC4=C3C=CC=C4)=N2)=C1)C5=CC=C(NC(/C=C/CN(C)C)=O)C=C5
MDL No. :MFCD28167785
InChI Key :OBJNFLYHUXWUPF-IZZDOVSWSA-N
Pubchem ID :73602827

Safety of THZ1

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of THZ1

Hedgehog

Isoform Comparison

Biological Activity

Description
THZ1 is a potent and selective covalent inhibitor of CDK7 with an IC50 of 3.2 nM, affecting CDK12 and CDK13 at higher concentrations and leading to the downregulation of MYC expression.

In Vitro:

Cell Line
Concentration Treated Time Description References
Jurkat cells 100 nM to 2 μM 6 hours Inhibition of CDK2 T-loop phosphorylation Cell Chem Biol. 2019 Jun 20;26(6):792-803.e10.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice A673 xenograft model Intraperitoneal (THZ1) and oral (olaparib) 10 mg/kg Twice daily for 40 days The combination of THZ1 and olaparib significantly inhibited tumor growth and extended survival without hematopoietic toxicity. Cancer Cell. 2018 Feb 12;33(2):202-216.e6.

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.77mL

0.35mL

0.18mL

8.83mL

1.77mL

0.88mL

17.67mL

3.53mL

1.77mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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