VTP50469

Catalog No.S8934

For research use only.

VTP50469 is a potent, highly selective and orally active inhibitor of Menin-MLL interaction with Ki of 104 pM. VTP50469 exhibits anti-leukemia activity.

VTP50469 Chemical Structure

CAS No. 2169916-18-9

Purity & Quality Control

Choose Selective MLL Inhibitors

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 Research:

[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 Research:

[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

Solubility (25°C)

In vitro

DMSO 100 mg/mL
(158.52 mM)
Water Insoluble
Ethanol '''100 mg/mL

Chemical Information

Molecular Weight 630.82
Formula

C32H47FN6O4S

CAS No. 2169916-18-9
Storage 3 years -20°C powder
2 years -80°C in solvent

In vivo Formulation Calculator (Clear solution)

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

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Molarity Calculator

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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