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THZ-1 hydrochloride

CAS No.

THZ-1 hydrochloride ( CDK7 inhibitor THZ1 )

Catalog No. M16941 CAS No.

THZ-1 hydrochloride is a potent, selective, covalent CDK7 inhibitor with IC50 of 3.2 nM; also weakly inhibits CDK12 with IC50 of 250 nM.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    THZ-1 hydrochloride
  • Note
    Research use only, not for human use.
  • Brief Description
    THZ-1 hydrochloride is a potent, selective, covalent CDK7 inhibitor with IC50 of 3.2 nM; also weakly inhibits CDK12 with IC50 of 250 nM.
  • Description
    THZ-1 hydrochloride is a potent, selective, covalent CDK7 inhibitor with IC50 of 3.2 nM; also weakly inhibits CDK12 with IC50 of 250 nM; displays broad-based activity a subset of cancer cell lines with IC50s of <200 nM; causes decreased cellular proliferation and an increase in apoptotic index (MCL-1, XIAP), disproportionally affects transcription of RUNX1 in Jurkat T-ALL cells; demonstrates efficacy against primary leukemia cells and in a bioluminescent xenografted model at 10mg/kg.
  • Synonyms
    CDK7 inhibitor THZ1
  • Pathway
    Angiogenesis
  • Target
    CDK
  • Recptor
    CDK
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    --
  • Formula Weight
    602.51
  • Molecular Formula
    C31H29Cl2N7O2
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO: 22.5 mg/mL
  • SMILES
    ——
  • Chemical Name
    Benzamide, N-[3-[[5-chloro-4-(1H-indol-3-yl)-2-pyrimidinyl]amino]phenyl]-4-[[(2E)-4-(dimethylamino)-1-oxo-2-buten-1-yl]amino]-, Hydrochloride

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Kwiatkowski N, et al. Nature. 2014 Jul 31;511(7511):616-20.
2. Chipumuro E, et al. Cell. 2014 Nov 20;159(5):1126-39.
3. Christensen CL, et al. Cancer Cell. 2014 Dec 8;26(6):909-22.
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