VTP50469 fumarate
Based on 13 publication(s) in Google Scholar
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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.79%
- No. CAS: 2169919-29-1
- Fòrmula: C32H47FN6O4S.3/2C4H4O4
- Peso molecular:804.93
-
Almacenamiento:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
-
Solvente y solubilidad
- Pureza y Documentación
- Referencias
-
Help & FAQs
Publications Citing Use of MedChemExpress (MCE) VTP50469 fumarate
More- Blood. 2026 Feb 24:blood.2025031486. [Abstract]
- Blood. 2024 Nov 7;144(19):2018-2032. [Abstract]
- Nat Cell Biol. 2023 Sep;25(9):1346-1358. [Abstract]
- Nat Commun. 2025 Mar 18;16(1):2641. [Abstract]
- Blood Cancer J. 2022 Jan 11;12(1):5. [Abstract]
- Leukemia. 2026 Mar 25. [Abstract]
- Leukemia. 2025 Jan;39(1):75-86. [Abstract]
- Blood Adv. 2026 Jul 14;10(13):4757-4771. [Abstract]
- Int J Oncol. 2020 Oct;57(4):1057-1071. [Abstract]
- bioRxiv. 2026 Jun 19.
- bioRxiv. 2026 Feb 17.
- bioRxiv. 2025 Nov 12:2025.11.10.687648. [Abstract]
- bioRxiv. 2023 Oct 1.
Customer Validation & Images
-
Cell Proliferation/Viability Assay
-
Cell Proliferation/Viability Assay
-
Cell Proliferation/Viability Assay
-
WB
-
WB
Actividad biológica
Descripciòn
IC50 & Target
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
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 2169919-29-1
-
Appearance Solid
-
Peso molecular 804.93
-
Fòrmula C32H47FN6O4S.3/2C4H4O4
-
Color White to off-white
-
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[C@H]5CC[C@H](NS(=O)(C)=O)CC5)CC4)C3.[3/2]
-
Synonyms
SNDX-50469 fumarate
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications (13)
-
Journal Impact Factor
-
Most Recent
-
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 Nov 7;144(19):2018-2032. PMID: 39158067 -
Nat Cell Biol
2023 Sep;25(9):1346-1358. PMID: 37591951
VTP50469 fumarate 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 fumarate 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 fumarate 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.
-
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 fumarate 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.
-
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 fumarate 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 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
2025 Nov 12:2025.11.10.687648. PMID: 41292793 -
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (124.23 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (3.11 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (3.11 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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.
Add each solvent one by one: 0.5% HPMC in Water
Solubility: 13.33 mg/mL (16.56 mM); Clear solution; Need ultrasonic
In Vivo Dissolution Calculator
Please enter the basic information of animal 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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
-
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)
-
Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.2423 mL | 6.2117 mL | 12.4234 mL | 31.0586 mL |
| 5 mM | 0.2485 mL | 1.2423 mL | 2.4847 mL | 6.2117 mL | |
| 10 mM | 0.1242 mL | 0.6212 mL | 1.2423 mL | 3.1059 mL | |
| 15 mM | 0.0828 mL | 0.4141 mL | 0.8282 mL | 2.0706 mL | |
| 20 mM | 0.0621 mL | 0.3106 mL | 0.6212 mL | 1.5529 mL | |
| 25 mM | 0.0497 mL | 0.2485 mL | 0.4969 mL | 1.2423 mL | |
| 30 mM | 0.0414 mL | 0.2071 mL | 0.4141 mL | 1.0353 mL | |
| 40 mM | 0.0311 mL | 0.1553 mL | 0.3106 mL | 0.7765 mL | |
| 50 mM | 0.0248 mL | 0.1242 mL | 0.2485 mL | 0.6212 mL | |
| 60 mM | 0.0207 mL | 0.1035 mL | 0.2071 mL | 0.5176 mL | |
| 80 mM | 0.0155 mL | 0.0776 mL | 0.1553 mL | 0.3882 mL | |
| 100 mM | 0.0124 mL | 0.0621 mL | 0.1242 mL | 0.3106 mL |
VTP50469 fumarate Related Classifications
HY-114162A Related Classifications
Powered by Bioz