For research use only. Not for therapeutic Use.
SY-5609(Cat No.:I044644)is a selective, non-covalent, and orally bioavailable inhibitor of cyclin-dependent kinase 7 (CDK7), with picomolar potency (Kd ≈ 0.065 nM). It disrupts transcriptional regulation and cell cycle progression by targeting CDK7’s roles in both the TFIIH complex and CDK-activating kinase (CAK). SY-5609 induces G2/M arrest and apoptosis in various cancer cell lines and demonstrates strong antitumor activity in xenograft models with favorable tolerability. It is currently in clinical trials for solid tumors, including KRAS-mutant cancers, and holds promise as a targeted therapy in transcription-driven malignancies.
CAS Number | 2417302-07-7 |
Synonyms | 7-dimethylphosphoryl-3-[2-[[(3S)-6,6-dimethylpiperidin-3-yl]amino]-5-(trifluoromethyl)pyrimidin-4-yl]-1H-indole-6-carbonitrile |
Molecular Formula | C23H26F3N6OP |
Purity | ≥95% |
IUPAC Name | 7-dimethylphosphoryl-3-[2-[[(3S)-6,6-dimethylpiperidin-3-yl]amino]-5-(trifluoromethyl)pyrimidin-4-yl]-1H-indole-6-carbonitrile |
InChI | InChI=1S/C23H26F3N6OP/c1-22(2)8-7-14(10-30-22)31-21-29-12-17(23(24,25)26)18(32-21)16-11-28-19-15(16)6-5-13(9-27)20(19)34(3,4)33/h5-6,11-12,14,28,30H,7-8,10H2,1-4H3,(H,29,31,32)/t14-/m0/s1 |
InChIKey | JDJOUBVVSQDIRC-AWEZNQCLSA-N |
SMILES | CC1(CC[C@@H](CN1)NC2=NC=C(C(=N2)C3=CNC4=C3C=CC(=C4P(=O)(C)C)C#N)C(F)(F)F)C |
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