THZ1 is a selective CDK7 inhibitor that preferentially diminishes transcription in cancer cells. THZ1 has the unprecedented ability to target a remote cysteine residue located outside of the canonical kinase domain, providing an unanticipated means of achieving selectivity for CDK7. Cancer cell-line profiling indicates that a subset of cancer cell lines, including human T-cell acute lymphoblastic leukaemia (T-ALL), have exceptional sensitivity to THZ1. Cyclin-dependent kinases (CDKs) are involved in temporal control of the cell cycle and transcription and play central roles in cancer development and metastasis.
MedKoo Cat#: 406560
Name: THZ1
CAS#: 1604810-83-4 (free base)
Chemical Formula: C31H28ClN7O2
Exact Mass: 565.1993
Molecular Weight: 566.05
Elemental Analysis: C, 65.78; H, 4.99; Cl, 6.26; N, 17.32; O, 5.65
| Solvent | mg/mL | mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 62.5 | 110.41 | |
| DMF | 30.0 | 53.00 | |
| DMF:PBS (pH 7.2) (1:2) | 0.3 | 0.53 |
The following data is based on the product molecular weight 566.05 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
