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THZ2

THZ2, an analogue of THZ1 with improved pharmacokinetic features, is a potent, selective CDK7 inhibitor with IC50 of 13.9 nM, displays a 5-fold improved half-life in vivo compared with THZ1; selectively targets CDK7 and potently inhibits the growth of triple-negative but not ER/PR+ breast cancer cells, efficiently suppresses the clonogenic growth of TNBC cells with IC50 of 10 nM; Like THZ1, THZ2 induces apoptotic cell death in triple-negative but not ER/PR+ breast cancer cells or normal human cells; suppresses the growth of triple-negative breast tumors in xenograft models.

Product Specifications

CAS Number

1604810-84-5

Product Name Alternative

THZ-2

Purity

>98% (HPLC)

Solubility

DMSO: ≥ 39 mg/mL

Smiles

O=C (NC1=CC=CC (NC2=NC=C (Cl) C (C3=CNC4=C3C=CC=C4) =N2) =C1) C5=CC=CC (NC (/C=C/CN (C) C) =O) =C5

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]-3-[[ (2E) -4- (dimethylamino) -1-oxo-2-buten-1-yl]amino]-

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