2098585-77-2
Chemical Structure
TAS1440
- CAS No.: 2098585-77-2
- Formula:C28H27F2N3O2
- Molecular Weight:475.53
InChIKey: SADVGAWKLORBLA-NRFANRHFSA-N
SMILES: N[C@H](C1)CCN1C(C(C=C2C3=CC=C(C#N)C(F)=C3)=CC=C2C4=CC=C(C=C4F)CC(C)(C)O)=O
Biological Activity: TAS1440 is an orally active LSD1/KDM1A inhibitor with a human IC50 of 4.8 nM. TAS1440 non-covalently binds to the histone H3-binding pocket of LSD1, inhibiting demethylase activity and disrupting repressive complexes with INSM1 and SMAD2. TAS1440 activates tumor-suppressive TGF-β and NOTCH signaling pathways via transcriptional reprogramming. TAS1440 can be used for the research of small cell lung cancer, specifically the SCLC-A subtype[1].
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TAS1440 | TAS1440 is an orally active LSD1/KDM1A inhibitor with a human IC50 of 4.8 nM. TAS1440 non-covalently binds to the histone H3-binding pocket of LSD1, inhibiting demethylase activity and disrupting repressive complexes with INSM1 and SMAD2. TAS1440 activates tumor-suppressive TGF-β and NOTCH signaling pathways via transcriptional reprogramming. TAS1440 can be used for the research of small cell lung cancer, specifically the SCLC-A subtype. | |||||||||||||||||||||
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Keywords
