THZ-1

CAS No. 1604810-83-4

THZ-1 ( CDK7 inhibitor )

Catalog No. M12303 CAS No. 1604810-83-4

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.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
5MG 73 In Stock
10MG 126 In Stock
25MG 215 In Stock
50MG 332 In Stock
100MG 448 In Stock
200MG Get Quote In Stock
500MG Get Quote In Stock
1G Get Quote In Stock

Biological Information

  • Product Name
    THZ-1
  • Note
    Research use only, not for human use.
  • Brief Description
    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.
  • Description
    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
  • Pathway
    Angiogenesis
  • Target
    CDK
  • Recptor
    CDK7
  • Research Area
    Cancer
  • Indication
    ——

Chemical Information

  • CAS Number
    1604810-83-4
  • Formula Weight
    566.05
  • Molecular Formula
    C31H28ClN7O2
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO: ≥ 27 mg/mL
  • SMILES
    CN(C)CC=CC(=O)NC1=CC=C(C=C1)C(=O)NC2=CC=CC(=C2)NC3=NC=C(C(=N3)C4=CNC5=CC=CC=C54)Cl
  • 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]-

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.
molnova catalog
related products
  • THZ-1 hydrochloride

    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.

  • Dalpiciclib

    Dalpiciclib is a highly selective, orally bioavailable, and comparable potency inhibitor of CDK4 and CKD6 with IC50s of 12.4?nM and 9.9?nM, respectively.

  • R-547

    A potent, selective and ATP-competitive CDK inhibitor with Ki of 1/3/1 nM for CDK1/2/4, respectively.