VTP50469

Catalog No.S8934 Batch:S893401

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Technical Data

Formula

C32H47FN6O4S
Molecular Weight 630.82 CAS No. 2169916-18-9
Solubility (25°C)* In vitro DMSO 100 mg/mL (158.52 mM)
Ethanol 100 mg/mL (158.52 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description VTP50469 is a potent, highly selective and orally active inhibitor of Menin-MLL interaction with Ki of 104 pM. VTP50469 exhibits anti-leukemia activity.
Targets
Menin-MLL interaction [1]
(Cell-free assay)
104 pM(Ki)

Biological Activity

Description VTP50469 is a potent, highly selective and orally active inhibitor of Menin-MLL interaction with Ki of 104 pM. VTP50469 exhibits anti-leukemia activity.
Targets
Menin-MLL interaction [1]
(Cell-free assay)
104 pM(Ki)
In vitro

Cell lines carrying MLL-rearrangements are selectively responsive to VTP50469. VTP50469 displaces Menin from protein complexes and inhibits chromatin occupancy of MLL at select genes. Loss of MLL binding leads to changes in gene expression, differentiation, and apoptosis.[2]
In vivo

Patient-derived xenograft (PDX) models derived from patients with either MLL-r AML or MLL-r ALL shows dramatic reductions of leukemia burden when treated with VTP50469. Multiple mice engrafted with MLL-r ALL remains disease free greater than one year after treatment.[2]

Protocol (from reference)

Cell Assay:

[2]
  • Cell lines

    MOLM13 cells, RS4;11 cells

  • Concentrations

    330 nM

  • Incubation Time

    2 and 7 days

  • Method

    In order to assess early and delayed gene expression changes, MOLM13 and RS4;11 cells are treated for 2 and 7 days with VTP50469 or DMSO followed by RNA-seq analysis.
Animal Study:

[2]
  • Animal Models

    7-9 week-old female NOD.Cg-PrkdcscidIl2rgtm1Wjl/SzJ (NSG) mice

  • Dosages

    15 mg/kg, 30 mg/kg, 60 mg/kg, 90 mg/kg, 120 mg/kg

  • Administration

    Oral gavage

Selleck's VTP50469 has been cited by 4 publications

Arachidonic acid released by PIK3CA mutant tumor cells triggers malignant transformation of colonic epithelium by inducing chromatin remodeling [ Cell Rep Med, 2024, S2666-3791(24)00179-4] PubMed: 38614093
MLL1 regulates cytokine-driven cell migration and metastasis [ Sci Adv, 2024, 10(11):eadk0785] PubMed: 38478601
Chemical-induced epigenome resetting for regeneration program activation in human cells [ Cell Rep, 2023, 42(6):112547] PubMed: 37224020
CRISPR-ChIP delineates a Menin-dependent oncogenic DOT1L complex in MLL-leukaemia [ bioRxiv, 2023, 10.1101/2023.03.17.533231] PubMed: None

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.