| Identification | Back Directory | [Name]
VTP50469 | [CAS]
2169916-18-9 | [Synonyms]
VTP50469
Benzamide, 5-fluoro-N,N-bis(1-methylethyl)-2-[[4-[7-[[trans-4-[(methylsulfonyl)amino]cyclohexyl]methyl]-2,7-diazaspiro[3.5]non-2-yl]-5-pyrimidinyl]oxy]- | [Molecular Formula]
C32H47FN6O4S | [MDL Number]
MFCD32197139 | [MOL File]
2169916-18-9.mol | [Molecular Weight]
630.82 |
| Chemical Properties | Back Directory | [Boiling point ]
735.2±70.0 °C(Predicted) | [density ]
1.28±0.1 g/cm3(Predicted) | [solubility ]
DMSO: Soluble: =10 mg/ml
Ethanol: Sparingly soluble: 1-10 mg/ml | [form ]
Solid | [pka]
10.97±0.40(Predicted) | [color ]
White to light yellow | [InChIKey]
ADHHOUXZPBYYSU-YOCNBXQISA-N | [SMILES]
C(N(C(C)C)C(C)C)(=O)C1=CC(F)=CC=C1OC1=CN=CN=C1N1CC2(CCN(C[C@@H]3CC[C@@H](NS(C)(=O)=O)CC3)CC2)C1 |
| Hazard Information | Back Directory | [Uses]
VTP50469 is a potent, highly selective and orally active Menin-MLL interaction inhibitor with a Ki of 104 pM. VTP50469 has potently anti-leukemia activity[1][2]. | [in vivo]
VTP50469 (15-60 mg/kg; oral administration; twice a day; for 28 days; NSG mice) treatment is highly efficacious across all dosage levels and all treatment groups have a significant survival advantage. Mice dosed at 30 and 60 mg/kg VTP50469 extends survival advantage[1]. | Animal Model: | Unconditioned immunodeficient (NSG) mice with MV4;11 cells[1] | | Dosage: | 15 mg/kg, 30 mg/kg, and 60 mg/kg | | Administration: | Oral administration; twice a day; for 28 days | | Result: | Was highly efficacious across all dosage levels and all treatment groups had a significant survival advantage over the control group.
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| [References]
[1] Krivtsov AV, et al. A Menin-MLL Inhibitor Induces Specific Chromatin Changes and Eradicates Disease in Models of MLL-Rearranged Leukemia. Cancer Cell. 2019 Dec 9;36(6):660-673.e11. DOI:10.1016/j.ccell.2019.11.001
[2] Andrei V. Krivtsov, et al. Abstract 4958: VTP50469 is a novel, orally available menin-MLL1 inhibitor effective against MLL-rearranged and NPM1-mutant leukemia. Cancer Resceach. July 2018.Volume 78, Issue 13 Supplement. |
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