THZ1 2HCl

CAS No. 2095433-94-4

THZ1 2HCl( THZ1 Dihydrochloride )

Catalog No. M28025 CAS No. 2095433-94-4

THZ1 2HCl is a selective, covalent, and allosteric inhibitor of CDK7 with an IC50 of 3.2 nM. THZ1 2HCl has antiproliferative effects on a variety of cancer cell lines.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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5MG 87 In Stock
10MG 151 In Stock
25MG 344 In Stock
50MG 462 In Stock
100MG 625 In Stock
200MG 927 In Stock
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Biological Information

  • Product Name
    THZ1 2HCl
  • Note
    Research use only, not for human use.
  • Brief Description
    THZ1 2HCl is a selective, covalent, and allosteric inhibitor of CDK7 with an IC50 of 3.2 nM. THZ1 2HCl has antiproliferative effects on a variety of cancer cell lines.
  • Description
    THZ1 2HCl is a selective, covalent, and allosteric inhibitor of CDK7 with an IC50 of 3.2 nM. THZ1 2HCl has antiproliferative effects on a variety of cancer cell lines.(In Vitro):THZ1 2HCl irreversibly inhibits the phosphorylation of RNA polymerase II CTD. THZ1 2HCl(250 nM) completely inhibits the phosphorylation of CDK7 substrate RNAPII CTD at Ser 5 and Ser 7, and the phosphorylation of Ser 2 is lost in Jurkat cells. Low concentrations of THZ1 2HCl have major effects on a small subset of genes, including RUNX1, thus leading to the subsequent loss of a larger gene expression program, resulting in cell death .(In Vivo):THZ1 2HCl inhibits the proliferation of KOPTK1 T-ALL cells in a mouse xenograft model. THZ1 2HCl(10 mg/kg) is well tolerated, and its body weight and behavior did not change significantly. THZ1 2HCl has no obvious toxic effects in animal models .
  • In Vitro
    ——
  • In Vivo
    ——
  • Synonyms
    THZ1 Dihydrochloride
  • Pathway
    Angiogenesis
  • Target
    CDK
  • Recptor
    CCR4
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2095433-94-4
  • Formula Weight
    638.98
  • Molecular Formula
    C31H30Cl3N7O2
  • Purity
    >98% (HPLC)
  • Solubility
    ——
  • SMILES
    O=C(NC1=CC=C(C(NC2=CC(NC3=NC(C4=CNC5=C4C=CC=C5)=C(Cl)C=N3)=CC=C2)=O)C=C1)C=CCN(C)C.Cl.Cl
  • Chemical Name
    ——

Shipping & Storage Information

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

Reference

1.Slack RJ, et al. Antagonism of human CC-chemokine receptor 4 can be achieved through three distinct binding sites on the receptor. Pharmacol Res Perspect. 2013 Dec;1(2):e00019.
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