Home Epigenetics MLL inhibitor - Histone Methyltransferase inhibitor VTP50469 For research use only.

VTP50469

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

VTP50469 Chemical Structure

CAS: 2169916-18-9

Selleck's VTP50469 has been cited by 2 publications

Purity & Quality Control

Batch: Purity: 99.99%
99.99

Products often used together with VTP50469

SB590885

VTP50469 and SB590885 are used in the induction medium to generate hCiPSCs from hADSCs and hASFs.

Deng H, et al. 2022.

SGC-CBP30

VTP50469 and SGC-CBP30 are used in the induction medium to generate hCiPSCs from hADSCs and hASFs.

Deng H, et al. 2022.

JNK-IN-8

VTP50469 and JNK-IN-8 are used in the induction medium to generate hCiPSCs from hADSCs and hASFs.

Deng H, et al. 2022.

Doramapimod (BIRB 796)

VTP50469 and Doramapimod are used in the induction medium to generate hCiPSCs from hADSCs and hASFs.

Deng H, et al. 2022.

Ruxolitinib

VTP50469 and Ruxolitinib are used in the induction medium to generate hCiPSCs from hADSCs and hASFs.

Deng H, et al. 2022.

VTP50469 Related Products

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
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]
Cell Research 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.
In Vivo
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]
Animal Research 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

Chemical Information & Solubility

Molecular Weight 630.82 Formula

C32H47FN6O4S
CAS No. 2169916-18-9 SDF --
Smiles CC(C)N(C(C)C)C(=O)C1=C(OC2=CN=CN=C2N3CC4(CCN(CC4)CC5CCC(CC5)N[S](C)(=O)=O)C3)C=CC(=C1)F
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (158.52 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble


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In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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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 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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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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