Referencia número: HY-114162

VTP50469

(Synonyms: SNDX-50469)

13 Cited Publications

Revisión del cliente

Based on 13 publication(s) in Google Scholar

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

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Pureza: 99.70%
No. CAS: 2169916-18-9
Fòrmula: C₃₂H₄₇FN₆O₄S
Peso molecular:630.82

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

VTP50469 Chemical Structure

No. CAS: 2169916-18-9

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (13)
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

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

IC₅₀ & Target

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

Ver todos los productos específicos de isoformas Epigenetic Reader Domain :

Cellular Effect

Cell Line	Type	Value	Description	References
MOLM-13	GI₅₀	13 nM Compound: 12; VTP50469	Antiproliferative activity against human MOLM-13 cells Antiproliferative activity against human MOLM-13 cells	[PMID: 34726905]
MV4-11	GI₅₀	17 nM Compound: 12; VTP50469	Antiproliferative activity against human MV4-11 cells Antiproliferative activity against human MV4-11 cells	[PMID: 34726905]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Chemical Information

No. CAS 2169916-18-9
Appearance Solid
Peso molecular 630.82
Fòrmula C₃₂H₄₇FN₆O₄S
Color White to light yellow
SMILES

O=C(N(C(C)C)C(C)C)C1=CC(F)=CC=C1OC2=CN=CN=C2N3CC4(CCN(C[C@H]5CC[C@H](NS(=O)(C)=O)CC5)CC4)C3
Synonyms

SNDX-50469
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (13)

All Cell Proliferation/Viability AssayWB

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Journal Impact Factor

Blood

Overcoming menin inhibitor resistance in AML cells with combinations including BET proteins and a dual BRG1/BRM inhibitor. [Abstract]

2026 Feb 24:blood.2025031486. PMID: 41734382
Blood

Epigenetic Regulation of Non-canonical Menin Targets Modulates Menin Inhibitor Response in Acute Myeloid Leukemia. [Abstract]

2024 Aug 16:blood.2023023644. PMID: 39158067
Nat Cell Biol

KDM6A epigenetically regulates subtype plasticity in small cell lung cancer. [Abstract]

2023 Sep;25(9):1346-1358. PMID: 37591951

VTP50469 purchased from MedChemExpress. Usage Cited in: Nat Cell Biol. 2023 Sep;25(9):1346-1358. [Abstract]

Immunoblot analysis of 1014 Kdm6a isogenic cells treated with inhibitors that block the function of epigenetic modifiers that normally maintain gene expression including VTP50469 (500 nM), EPZ-5676 (1 μM), PF-9363 (100 nM), JQAD1 or DMSO for 6 days.
Nat Commun

Guanine nucleotide biosynthesis blockade impairs MLL complex formation and sensitizes leukemias to menin inhibition. [Abstract]

2025 Mar 18;16(1):2641. PMID: 40102405

VTP50469 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Mar 18;16(1):2641. [Abstract]

Relative viability of MOLM-13 cells following treatment with different concentrations of VTP50469 (3.91-1000 nM) over 2-7 days.

VTP50469 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Mar 18;16(1):2641. [Abstract]

Relative viability of human AML cell lines upon treatment with different concentrations of VTP50469 (3.91-1000 nM) over 5 days.
Leukemia

A Perturb-seq map of a differentiation hub reveals synergistic vulnerabilities in KMT2A-rearranged acute myeloid leukemia. [Abstract]

2026 Mar 25. PMID: 41882099
Leukemia

NPM1-fusion proteins promote myeloid leukemogenesis through XPO1-dependent HOX activation. [Abstract]

2025 Jan;39(1):75-86. PMID: 39443736

VTP50469 purchased from MedChemExpress. Usage Cited in: Leukemia. 2025 Jan;39(1):75-86. [Abstract]

NPM1::CCDC28A cells and mouse cKit+ bone marrow cells were incubated with selinexor or VTP50469 (0, 0.1, 0.3, 1, 3, 10, and 30 μM) at the indicated concentration for 72 h. Cell viability was assessed using the Cell Counting Kit-8.
Blood Cancer J

Effective Menin inhibitor-based combinations against AML with MLL rearrangement or NPM1 mutation (NPM1c). [Abstract]

2022 Jan 11;12(1):5. PMID: 35017466

VTP50469 purchased from MedChemExpress. Usage Cited in: Blood Cancer J. 2022 Jan 11;12(1):5. [Abstract]

A, B MOLM13 and OCI-AML3 cells were treated with the indicated concentrations of VTP50469 (SNDX-50469; 0, 0.25, 1 μM) for 48 h. Following this, total cell lysates were prepared and immunoblot analyses were conducted. The expression levels of β-Actin in the lysates served as the loading control.
Blood Adv

Combining menin and MEK inhibition to target poor prognosis KMT2A-rearranged RAS pathway-mutant acute myeloid leukemia. [Abstract]

2026 Jul 14;10(13):4757-4771. PMID: 42085603
Int J Oncol

Menin‑MLL inhibitors induce ferroptosis and enhance the anti‑proliferative activity of auranofin in several types of cancer cells. [Abstract]

2020 Oct;57(4):1057-1071. PMID: 32945449
bioRxiv

2026 Jun 19.
bioRxiv

2026 Feb 17.
bioRxiv

Menin inhibition impairs metastatic colonization of Ewing sarcoma. [Abstract]

2025 Nov 12:2025.11.10.687648. PMID: 41292793
bioRxiv

2023 Oct 1.

Solvente y solubilidad

In Vitro:

DMSO : 100 mg/mL (158.52 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.5852 mL

7.9262 mL

15.8524 mL

5 mM

0.3170 mL

1.5852 mL

3.1705 mL

10 mM

0.1585 mL

0.7926 mL

1.5852 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculadora de molaridad

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline

Solubility: ≥ 2.5 mg/mL (3.96 mM); Clear solution

Protocol 2

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (3.96 mM); Clear solution

Protocol 3

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (3.30 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 4

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (3.30 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 5

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (3.30 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (280 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Krivtsov AV, et al. A Menin-MLL Inhibitor Induces Specific Chromatin Changes and Eradicates Disease in Models of MLL-Rearranged Leukemia. Cancer Cell. 2019 Dec 9;36(6):660-673.e11. [Content Brief]

[2]. Andrei V. Krivtsov, et al. Abstract 4958: VTP50469 is a novel, orally available menin-MLL1 inhibitor effective against MLL-rearranged and NPM1-mutant leukemia. Cancer Resceach. July 2018.Volume 78, Issue 13 Supplement.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.5852 mL	7.9262 mL	15.8524 mL	39.6310 mL
	5 mM	0.3170 mL	1.5852 mL	3.1705 mL	7.9262 mL
	10 mM	0.1585 mL	0.7926 mL	1.5852 mL	3.9631 mL
	15 mM	0.1057 mL	0.5284 mL	1.0568 mL	2.6421 mL
	20 mM	0.0793 mL	0.3963 mL	0.7926 mL	1.9815 mL
	25 mM	0.0634 mL	0.3170 mL	0.6341 mL	1.5852 mL
	30 mM	0.0528 mL	0.2642 mL	0.5284 mL	1.3210 mL
	40 mM	0.0396 mL	0.1982 mL	0.3963 mL	0.9908 mL
	50 mM	0.0317 mL	0.1585 mL	0.3170 mL	0.7926 mL
	60 mM	0.0264 mL	0.1321 mL	0.2642 mL	0.6605 mL
	80 mM	0.0198 mL	0.0991 mL	0.1982 mL	0.4954 mL
	100 mM	0.0159 mL	0.0793 mL	0.1585 mL	0.3963 mL

Keywords

VTP50469

13 Cited Publications

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VTP50469

MCE Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) VTP50469

Ver todos los productos específicos de isoformas Epigenetic Reader Domain

Actividad biológica

Chemical Information

Publications (13)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

VTP50469

MCE Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) VTP50469

Ver todos los productos específicos de isoformas Epigenetic Reader Domain

Actividad biológica

Chemical Information

Publications (13)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

VTP50469 Related Classifications

HY-114162 Related Classifications