1. Epigenetics
    Apoptosis
  2. Epigenetic Reader Domain
    Apoptosis
  3. VTP50469 fumarate

VTP50469 fumarate 

Cat. No.: HY-114162A
Handling Instructions

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

For research use only. We do not sell to patients.

VTP50469 fumarate Chemical Structure

VTP50469 fumarate Chemical Structure

CAS No. : 2169919-29-1

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Description

VTP50469 fumarate is a potent, highly selective and orally active Menin-MLL interaction inhibitor with a Ki of 104 pM. VTP50469 fumarate has potently anti-leukemia activity[1][2].

IC50 & Target

Ki: 104 pM (Menin-MLL interaction)[1][2]

In Vitro

VTP50469 more potently and rapidly inhibits cell proliferation in a concentration-dependent manner in MLL-r cell lines carrying (MOLM13 (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)) 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[1].
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[1].
VTP50469 displaces Menin from protein complexes and inhibits chromatin occupancy of MLL at select genes. Loss of MLL binding led to changes in gene expression, differentiation, and apoptosis[1].

In Vivo

VTP50469 (15-60 mg/kg; oral administration; twice a day; for 28 days; NSG mice) 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].

Animal Model: Unconditioned immunodeficient (NSG) mice with MV4;11 cells[1]
Dosage: 15 mg/kg, 30 mg/kg, and 60 mg/kg
Administration: Oral administration; twice a day; for 28 days
Result: Was highly efficacious across all dosage levels and all treatment groups had a significant survival advantage over the control group.
Molecular Weight

804.93

Formula

C₃₂H₄₇FN₆O₄S.₃/₂C₄H₄O₄

CAS No.

2169919-29-1

SMILES

O=C(O)/C=C/C(O)=O.O=C(N(C(C)C)C(C)C)C1=CC(F)=CC=C1OC2=CN=CN=C2N3CC4(CCN(C[[email protected]]5CC[[email protected]](NS(=O)(C)=O)CC5)CC4)C3.[3/2]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

VTP50469VTP 50469VTP-50469Epigenetic Reader DomainApoptosisMenin-MLLprotein-proteinleukemiaantiproliferativedifferentiationapoptosissurvivalInhibitorinhibitorinhibit

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VTP50469 fumarate
Cat. No.:
HY-114162A
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