Home Tools
Log in
Cart

THZ2

Catalog No. T7296   CAS 1604810-84-5
Synonyms: CDK7-IN-1

THZ2 (CDK7-IN-1), an analog of THZ1, is a potent and selective CDK7 inhibitor(IC50:13.9 nM),with the potential to treat Triple-negative breast cancer (TNBC).

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
THZ2 Chemical Structure
THZ2, CAS 1604810-84-5
Pack Size Availability Price/USD Quantity
1 mg In stock $ 93.00
5 mg In stock $ 197.00
10 mg In stock $ 272.00
25 mg In stock $ 493.00
50 mg In stock $ 719.00
100 mg In stock $ 987.00
1 mL * 10 mM (in DMSO) In stock $ 248.00
Bulk Inquiry
Get quote
Select Batch  
Purity: 98%
Contact us for more batch information
Biological Description
Chemical Properties
Storage & Solubility Information
Description THZ2 (CDK7-IN-1), an analog of THZ1, is a potent and selective CDK7 inhibitor(IC50:13.9 nM),with the potential to treat Triple-negative breast cancer (TNBC).
Targets&IC50 CDK7:13.9 nM
In vitro The survivals of all six cell lines were decreased in a dose-dependent manner after THZ2 treatment. GES-1 cells were most insensitive to THZ2 with the highest IC50 values of 2.45 μM. The IC50 values of THZ2 in AGS, BGC-823, MGC-803, MKN-45 and SGC-7901 were 0.19 μM, 0.69 μM, 0.74 μM, 0.73 μM and 0.68 μM respectively, which were positively correlated with the protein expression of CDK7 in these cells[1].
In vivo Generated the xenograft tumor models by transplanting BGC-823 cells into nude mice. Compared with the control group, treatment with THZ2 significantly inhibited the growth of BGC-823 tumors by diminishing the volume and weight of tumors, but did not change the the weight of nude mice. The inhibition rate of tumor growth in THZ2 treatment group was 44.00%[1].
Cell Research Cells were firstly seeded into a 96-well plate at a density of 3000 cells per well, and incubated with THZ2 in three parallel wells for 72 h. Then MTT was added to each well at a final concentration of 0.5 mg/ml. After incubation for 4 h, formazan crystals were dissolved in 100 μl of DMSO, and absorbance at 570 nm was measured by plate reader. The concentrations required to inhibit growth by 50% (IC50) were calculated from survival curves using the Bliss method[1].
Animal Research Balb/c nude mice feed on sterilized food and water. Six female nude mice with 5 weeks old were used for two groups. Each mouse was injected subcutaneously with BGC-823 cells (3 × 10^6 in 100 μl of medium) under the shoulder. When the subcutaneous tumors were approximately 0.3 × 0.3 cm^2 (two perpendicular diameters) in size, mice were randomized into two groups, and were injected intraperitoneally with vehicle alone (0.9% saline) and THZ2 (10 mg/kg) once/day at first 16 days and twice/day at last 6 days. The body weights of mice and the two perpendicular diameters (A and B) of tumors were recorded. The tumor volume (V) was calculated according to the formula: V = (π/6) × [(A+B)/2]^3. The mice were anaesthetized after experiment, and tumor tissue was excised from the mice and weight. The rate of inhibition (IR) was calculated according to the formula: IR = [1 - (Mean tumor weight of experimental group/Mean tumor weight of control group)] × 100%[1].
Synonyms CDK7-IN-1
Molecular Weight 566.05
Formula C31H28ClN7O2
CAS No. 1604810-84-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 39 mg/mL (68.90 mM)

TargetMolReferences and Literature

1. Huang JR, Qin WM, Wang K,et al.Cyclin-dependent kinase 7 inhibitor THZ2 inhibits the growth of human gastric cancer in vitro and in vivo.Am J Transl Res. 2018 Nov 15;10(11):3664-3676. 2. CDK7-dependent transcriptional addiction in triple-negative breast cancer.

TargetMolCitations

1. Jiang L, Yu Y, Li Z, et al.BMS-265246, a Cyclin-Dependent Kinase Inhibitor, Inhibits the Infection of Herpes Simplex Virus Type 1.Viruses.2023, 15(8): 1642.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library Anti-Breast Cancer Compound Library Anti-Aging Compound Library Anti-Pancreatic Cancer Compound Library Covalent Inhibitor Library NO PAINS Compound Library Bioactive Compounds Library Max Anti-Cancer Compound Library Kinase Inhibitor Library Bioactive Compound Library

Related Products

Related compounds with same targets
IC261 Bromosporine XY028-140 H1k CDK-IN-2 CLK1/2-IN-3 CGP60474 ZCL278

TargetMolDose Conversion

You can also refer to dose conversion for different animals. More

TargetMol In vivo Formulation Calculator (Clear solution)

Step One: Enter information below
Dosage
mg/kg
Average weight of animals
g
Dosing volume per animal
ul
Number of animals
Step Two: Enter the in vivo formulation
% DMSO
%
% Tween 80
% ddH2O
Calculate Reset

TargetMolCalculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculation
Molecular Weight Calculator
=
X
X

Molarity Calculator allows you to calculate the

  • Mass of a compound required to prepare a solution of known volume and concentration
  • Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Concentration of a solution resulting from a known mass of compound in a specific volume
See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

X
=
X

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

=
/

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

THZ2 1604810-84-5 Cell Cycle/Checkpoint CDK inhibit THZ 2 Cyclin dependent kinase THZ-2 CDK7-IN-1 Inhibitor inhibitor

 

TargetMol