VTP50469 NEW
| Price | $176 | $372 | $446 |
| Package | 1mg | 5mg | 10mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-19 |
Product Details
| Product Name: VTP50469 | CAS No.: 2169916-18-9 |
| Purity: 98.92% | Supply Ability: 10g |
| Release date: 2024/11/19 |
Product Introduction
Bioactivity
| Name | VTP50469 |
| Description | VTP50469 is a highly selective and orally active small molecule inhibitor of the Menin-MLL protein-protein interaction with potent anti-leukemic activity with a Ki of 104 pM. |
| In vitro | VTP50469 inhibits cell proliferation in a concentration-dependent manner in MLL-r cell lines, including (MOLM13 with IC50 of 13 nM), THP1 (IC50 of 37 nM), NOMO1 (IC50 of 30 nM), ML2 (IC50 of 16 nM), EOL1 (IC50 of 20 nM), and murine MLL-AF9 cells (IC50 of 15 nM)), as well as ALL cell lines (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)). At early timepoints, MLL-r B cell ALL (B-ALL) cell lines, but not MLL-r AML cell lines, underwent dose-dependent apoptosis in response to VTP50469, while MLL-r AML cell lines exhibited dose-dependent differentiation starting at 4-6 days of exposure. VTP50469 displaces Menin from protein complexes, reducing MLL chromatin occupancy on certain genes, resulting in altered gene expression, differentiation, and apoptosis [1]. |
| In vivo | METHODS: MV4-transplanted NSG mice were treated with VTP50469 (15, 30, and 60 mg/kg, orally twice a day) and the tumor growth in vivo was observed. RESULTS The size of subcutaneous tumors in mice decreased in a dose-dependent manner. [1] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 125 mg/mL (198.15 mM), Sonication is recommended. |
| Keywords | Menin-MLL | leukemia | survival | Epigenetic Reader Domain | antiproliferative | Apoptosis | Inhibitor | protein-protein | VTP-50469 | VTP50469 | inhibit | VTP 50469 | differentiation |
| Inhibitors Related | Stavudine | 5-Fluorouracil | Acetylcysteine | Kaempferol | Myricetin | Sodium 4-phenylbutyrate | L-Ascorbic acid | Dextran sulfate sodium salt (MW 4500-5500) | Metronidazole | Sorafenib | Tributyrin | Curcumin |
| Related Compound Libraries | Highly Selective Inhibitor Library | Histone Modification Compound Library | Bioactive Compound Library | Epigenetics Compound Library | Inhibitor Library | NO PAINS Compound Library | PPI Inhibitor Library | Orally Active Compound Library | Bioactive Compounds Library Max | Anti-Cancer Active Compound Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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United States- Since: 2011-01-07
- Address: 36?Washington?Street, Wellesley?Hills
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