THZ2 is a potent and selective CDK7 inhibitor with the potential to treat Triple-negative breast cancer. THZ2 at low nanomolar doses efficiently suppresses the clonogenic growth of TNBC cells with IC50 of appr 10 nM. THZ2 induces apoptotic cell death in triple-negative but not ER/PR+ breast cancer cells or normal human cells.
In vivo, THZ2 (10 mg/Kg) markedly reduces the growth rate of tumors in mice and demonstrates an anti-tumor activity. THZ2 in NOD-SCID mice leads to reduced body weight, suggesting that THZ2 mayt be less well-tolerated in this particular mouse strain.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO: ≥ 30 mg/mL|
Human TFIIH Kinase CDK7 Regulates Transcription-Associated Chromatin Modifications.
Ebmeier CC, et al. Cell Rep. 2017 Aug 1;20(5):1173-1186. PMID: 28768201.
Preclinical Efficacy and Molecular Mechanism of Targeting CDK7-Dependent Transcriptional Addiction in Ovarian Cancer.
Zhang Z, et al. Mol Cancer Ther. 2017 Sep;16(9):1739-1750. PMID: 28572168.
CDK7-dependent transcriptional addiction in triple-negative breast cancer.
Wang Y, et al. Cell. 2015 Sep 24;163(1):174-86. PMID: 26406377.
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