2892631-70-6
Chemical Structure
PF15
- CAS No.: 2892631-70-6
- Formula:C44H49N13O6
- Molecular Weight:855.94
IUPAC Name: 2-(4-isobutylphenyl)-N-(5-(propylthio)-1,3,4-thiadiazol-2-yl)propanamide
InChIKey: BQDQZCCNJKVYDD-UHFFFAOYSA-N
SMILES: CC(C)(C1=CC(NC(NC2=CC=C(C=C2)C3=CN(C4=NC=NC(N)=C34)CCCCC5=CN(N=N5)CCCCC(NC6=C7CN(C(C7=CC=C6)=O)C8CCC(NC8=O)=O)=O)=O)=NO1)C
Biological Activity: PF15 is an orally active FLT3-ITD PROTAC degrader with a DC50 of 76.7 nM and an IC50 of 36 nM against FLT3-ITD. PF15 induces FLT3-ITD protein degradation, thereby downregulating its phosphorylation level. PF15 inhibits the proliferation of FLT3-ITD-positive cells and reduces the phosphorylation level of STAT5, a downstream molecule of FLT3-ITD. PF15 exhibits efficacy in in vivo xenograft models of acute myeloid leukemia and prolongs survival. PF15 can be used for the research of acute myeloid leukemia[1].
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PF15 | PF15 is an orally active FLT3-ITD PROTAC degrader with a DC50 of 76.7 nM and an IC50 of 36 nM against FLT3-ITD. PF15 induces FLT3-ITD protein degradation, thereby downregulating its phosphorylation level. PF15 inhibits the proliferation of FLT3-ITD-positive cells and reduces the phosphorylation level of STAT5, a downstream molecule of FLT3-ITD. PF15 exhibits efficacy in in vivo xenograft models of acute myeloid leukemia and prolongs survival. PF15 can be used for the research of acute myeloid leukemia. | |||||||||||||||||||||
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