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THZ-1

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.

Product Specifications

CAS Number

1604810-83-4

Product Name Alternative

CDK7 inhibitor

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

Molecular Formula

C31H28ClN7O2

Molecular Weight

566.0527

Storage Conditions

Storage temperature: -20°C. Stability: ≥ 2 years

Notes

For research use only.

Other Product Names

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]-

Available Sizes

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