THZ2

Catalog No.S7969 Batch:S796901

Technical Data

Formula

C₃₁H₂₈ClN₇O₂

Molecular Weight

566.05

CAS No.

1604810-84-5

Solubility (25°C)*

In vitro

DMSO

100 mg/mL (176.66 mM)

Water

˂1 mg/mL

Ethanol

˂1 mg/mL

In vivo (Add solvents to the product individually and in order)

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5mg/ml (8.83mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.71mg/ml (1.25mM)	Taking the 1 mL working solution as an example, add 50 μL of 14.2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

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.

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. This compound 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 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.

Protocol (from reference)

Cell Assay:^{^[1]}	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.
Animal Study:^{^[1]}	Animal Models Nude mice (Foxn1nu) Dosages 10 mg/kg Administration IP

Cell Assay:^{^[1]}

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.

Animal Study:^{^[1]}

Animal Models
Nude mice (Foxn1nu)
Dosages
10 mg/kg
Administration
IP

References

https://pubmed.ncbi.nlm.nih.gov/26406377/

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.