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VTP50469

Catalog No. T13336 CAS 2169916-18-9

VTP50469 is a highly selective and orally active inhibitor of Menin-MLL interaction( Ki: 104 pM) and has potently anti-leukemia activity.

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VTP50469, CAS 2169916-18-9

Pack Size	Availability	Price/USD
1 mg	In stock	$ 177.00
5 mg	In stock	$ 374.00
10 mg	In stock	$ 597.00
25 mg	In stock	$ 964.00
50 mg	In stock	$ 1,290.00
100 mg	In stock	$ 1,760.00
200 mg	In stock	$ 2,370.00
1 mL * 10 mM (in DMSO)	In stock	$ 519.00

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Purity: 98.92%

Purity: 98.31%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	VTP50469 is a highly selective and orally active inhibitor of Menin-MLL interaction( Ki: 104 pM) and has potently anti-leukemia activity.
Targets&IC50	Menin-MLL:ki:104 pM
In vitro	VTP50469 more potently and rapidly inhibits cell proliferation in a concentration-dependent manner in MLL-r cell lines carrying (MOLM13 with IC50 of 13 nM), THP1 with IC50 of 37 nM, NOMO1 with IC50 of 30 nM, ML2 (IC50 of 16 nM), EOL1 (IC50 of 20 nM), and murine MLL-AF9 cells (IC50 of 15 nM)) and ALL (KOPN8 (IC50 of 15 nM), HB11;19 (IC50 of 36 nM), MV4;11 (IC50 of 17 nM), SEMK2 (IC50 of 27 nM), and RS4;11 (IC50 of 25 nM)) cell lines. At early timepoints MLL-r B cell ALL (B-ALL) cell lines, but not MLL-r AML cell lines, underwent apoptosis in response to VTP50469 in a dose-dependent manner. MLL-r AML cell lines underwent dose-dependent differentiation starting at 4-6 days of exposure to VTP50469. VTP50469 replaces Menin in protein complexes and suppresses the chromatin occupancy of MLL on certain genes. Loss of MLL binding leads to changes in gene expression, differentiation, and apoptosis [1].
In vivo	In NSG mice, VTP50469 (15-60 mg/kg; p.o.; twice a day; for 28 days) 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].

Molecular Weight	630.82
Formula	C32H47FN6O4S
CAS No.	2169916-18-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 125 mg/mL (198.15 mM), Sonication is recommended.

References and Literature

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. 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.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Inhibitor Library Highly Selective Inhibitor Library Epigenetics Compound Library Preclinical Compound Library Hematonosis Compound Library ReFRAME Related Library Reprogramming Compound Library Anti-Cancer Compound Library PPI Inhibitor Library

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

VTP50469 2169916-18-9 Apoptosis Chromatin/Epigenetic Epigenetic Reader Domain Histone Methyltransferase Menin-MLL leukemia survival antiproliferative Inhibitor protein-protein VTP-50469 inhibit VTP 50469 differentiation inhibitor

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