THZ531 is a covalent CDK12 and CDK13 inhibitor with IC50 values of 158 nM and 69 nM, respectively. THZ531 irreversibly targets a cysteine located outside the kinase domain. THZ531 causes a loss of gene expression with concurrent loss of elongating and hyperphosphorylated RNA polymerase II. THZ531 substantially decreases the expression of DNA damage response genes and key super-enhancer-associated transcription factor genes.
*This compound is unstable in solutions, freshly prepared is recommended.
Molecular Weight | 558.07 |
Formula | C30H32ClN7O2 |
CAS Number | 1702809-17-3 |
Solubility (25°C) | DMSO ≥ 12 mg/mL |
Storage | -20°C, dry, sealed, protect from light |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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