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THZ2

Cat. No. M8995
THZ2 Structure
Size Price Availability Quantity
5mg USD 340 In stock
10mg USD 500 In stock
50mg USD 1450 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control
  • Current batch:
  • Purity >97%
  • COA
  • MSDS
Biological Activity

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 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.

Chemical Information
Molecular Weight 566.05
Formula C31H28ClN7O2
CAS Number 1604810-84-5
Purity >97%
Solubility DMSO: ≥ 30 mg/mL
Storage at -20°C
References

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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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: THZ2 supplier, CDK, inhibitors

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