2169916-18-9
VTP50469
CAS: 2169916-18-9
Molecular Formula: C32H47FN6O4S
2169916-18-9 - Names and Identifiers
| Name | VTP50469 |
| 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]- |
| CAS | 2169916-18-9 |
2169916-18-9 - Physico-chemical Properties
| Molecular Formula | C32H47FN6O4S |
| Molar Mass | 630.82 |
| Solubility | Soluble in DMSO |
| Storage Condition | -20°C |
| Use | VTP50469 is a potent, highly selective and orally active inhibitor of Menin-MLL interaction with Ki of 104 pM. VTP50469 exhibits anti-leukemia activity. |
2169916-18-9 - Reference
| Reference Show more | 1: Kurmasheva RT, Bandyopadhyay A, Favours E, Pozo VD, Ghilu S, Phelps DA, McGeehan GM, Erickson SW, Smith MA, Houghton PJ. Evaluation of VTP-50469, a menin-MLL1 inhibitor, against Ewing sarcoma xenograft models by the pediatric preclinical testing consortium. Pediatr Blood Cancer. 2020 Jul;67(7):e28284. doi: 10.1002/pbc.28284. Epub 2020 Apr 25. PMID: 32333633. 2: Gundry MC, Goodell MA, Brunetti L. It's All About MEis: Menin-MLL Inhibition Eradicates NPM1-Mutated and MLL-Rearranged Acute Leukemias in Mice. Cancer Cell. 2020 Mar 16;37(3):267-269. doi: 10.1016/j.ccell.2020.02.011. PMID: 32183947. 3: Uckelmann HJ, Kim SM, Wong EM, Hatton C, Giovinazzo H, Gadrey JY, Krivtsov AV, Rücker FG, Döhner K, McGeehan GM, Levine RL, Bullinger L, Vassiliou GS, Armstrong SA. Therapeutic targeting of preleukemia cells in a mouse model of NPM1 mutant acute myeloid leukemia. Science. 2020 Jan 31;367(6477):586-590. doi: 10.1126/science.aax5863. PMID: 32001657; PMCID: PMC7754791. 4: Krivtsov AV, Evans K, Gadrey JY, Eschle BK, Hatton C, Uckelmann HJ, Ross KN, Perner F, Olsen SN, Pritchard T, McDermott L, Jones CD, Jing D, Braytee A, Chacon D, Earley E, McKeever BM, Claremon D, Gifford AJ, Lee HJ, Teicher BA, Pimanda JE, Beck D, Perry JA, Smith MA, McGeehan GM, Lock RB, Armstrong SA. 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. PMID: 31821784; PMCID: PMC7227117. |
2169916-18-9 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.585 ml | 7.926 ml | 15.852 ml |
| 5 mM | 0.317 ml | 1.585 ml | 3.17 ml |
| 10 mM | 0.159 ml | 0.793 ml | 1.585 ml |
| 5 mM | 0.032 ml | 0.159 ml | 0.317 ml |
Last Update：2024-01-02 23:10:35
2169916-18-9 - Reference Information
| uses | VTP50469 is a small molecule inhibitor of Menin-MLL protein-protein interactions. |
| biological activity | VTP50469 is a potent, highly selective and orally active inhibitor of Menin-MLL interaction, ki value was 104 pM. VTP50469 has anti-leukemia activity. |
| Target | TargetValue Menin-MLL interaction (Cell-free assay) 104 pM(Ki) |
| Target | Value |
| Menin-MLL interaction (Cell-free assay) | 104 pM(Ki) |
Last Update：2024-04-09 21:54:55
