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VTP50469 Menin-MLL Inhibitor

Name: VTP50469
Brand: Selleck Chemicals
SKU: S8934
Availability: InStock
Rating: 5 (7 reviews)

Cat.No.S8934

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

Chemical Structure

Molecular Weight: 630.82

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.99%

99.99

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Related Targets	Epigenetic Reader Domain HDAC JAK Histone Methyltransferase AMPK PKC PARP HIF Histone Acetyltransferase Aurora Kinase Sirtuin PRMT Histone Demethylase EZH1/2 DNA Methyltransferase Pim LSD1 JMJD G9a/GLP NSD FTO MicroRNA PAD SETD SMYD DOT1 COMT WDR5 HNMT SAM MTase

Chemical Information, Storage & Stability

Molecular Weight	630.82	Formula	C₃₂H₄₇FN₆O₄S	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	2169916-18-9	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			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

Solubility

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

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.670mg/ml (2.65mM)	Taking the 1 mL working solution as an example, add 50 μL of 33.3 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to make it clear. Volume up to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

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.

Mechanism of Action

Targets/IC₅₀/Ki	Menin-MLL interaction ^[1] (Cell-free assay) 104 pM(Ki)
In vitro	Cell lines carrying MLL-rearrangements are selectively responsive to VTP50469. This compound 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 with this compound.^[2]
References	https://cancerres.aacrjournals.org/content/78/13_Supplement/4958 https://pubmed.ncbi.nlm.nih.gov/31821784/

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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