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VTP50469

Chemical Structure : VTP50469

CAS No.: 2169916-18-9

VTP50469 (VTP 50469, VTP-50469, SNDX-50469)

Catalog No.: PC-72792Not For Human Use, Lab Use Only.

VTP50469 (VTP 50469) is potent, selective, orally active inhibitor of Menin-MLL interaction with Ki of 104 pM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

VTP50469 (VTP 50469, SNDX-50469) is potent, selective, orally active inhibitor of Menin-MLL interaction with Ki of 104 pM.
VTP50469 treatment led to a profound reduction in cell proliferation in a concentration-dependent manner in MLL-r cell lines carrying but not in those with WT MLL (HL-60, REH, K562, murine MOZ-TIF2).
VTP50469 treatment rapidly suppresses MLL-fusion target gene expression, induces global changes in Menin and selective changes in MLL chromatin occupancy.
VTP50469 treatment can eradicate disease in PDX models of MLL-r acute leukemia.

Physicochemical Properties

M.Wt 630.3364
Formula C32H47FN6O4S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

5-Fluoro-N,N-diisopropyl-2-((4-(7-(((1r,4r)-4-(methylsulfonamido)cyclohexyl)methyl)-2,7-diazaspiro[3.5]nonan-2-yl)pyrimidin-5-yl)oxy)benzamide

References

1. Krivtsov AV, et al. Cancer Cell. 2019 Dec 9;36(6):660-673.e11.

2. Heikamp EB, et al. Blood. 2021 Sep 28:blood.2021012806.

3. Warren Fiskus, et al. Blood Cancer J. 2022 Jan 11;12(1):5.

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