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
* <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.)

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Biological Activity

Description

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.

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. THZ2 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 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.^[1]

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

[1] Yubao Wang, et al. Cell. 2015 Sep 24;163(1):174-86.

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SHIPPING AND STORAGE
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