VTP-50469 is a novel, potent, selective, orally-available Menin MLL1 inhibitor, being effectively against MLL-rearranged and NPM1c+ leukemia, selectively killing cell lines with MLL rearrangements and NPM1c+ mutations. Cell lines carrying MLL rearrangements were selectively responsive to VTP50469. VTP50469 displaced Menin from protein complexes and inhibited chromatin occupancy of MLL at select genes. Loss of MLL binding led to changes in gene expression, differentiation, and apoptosis. Patient-derived xenograft (PDX) models derived from patients with either MLL-r acute myeloid leukemia or MLL-r acute lymphoblastic leukemia (ALL) showed dramatic reductions of leukemia burden when treated with VTP50469.
Cat.No
DC75761
Name
VTP50469 free base
Chemical Properties
CAS
2169916-18-9
Formula
C32H47FN6O4S
MW
630.824
Storage
2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
References
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