Gintemetostat
Based on 1 publication(s) in Google Scholar
Gintemetostat (KTX-1001) is an orally active, highly specific NSD2/MMSET histone methyltransferase inhibitor with human NSD2 IC50 values ranging 0.460-2.17 nM and NSD2 SET domain IC50 of 2.32 nM and Kd values ranging 6.3-70.4 nM.Gintemetostat reduces H3K36me2 levels, impairs multiple myeloma cell adhesion and colony formation, enhances cytotoxicity, boosts T-cell activation, and sensitizes resistant multiple myeloma cells to other agents.Gintemetostat can be used for the research of multiple myeloma and relapsed and refractory multiple myeloma.
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- Pureza: 99.81%
- No. CAS: 2604513-16-6
- Fòrmula: C25H26F4N8O2
- Peso molecular:546.52
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Gintemetostat
MoreVer todos los productos específicos de isoformas Histone Methyltransferase
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Actividad biológica
Combination treatment with Gintemetostat (0.5-2.5 μM) and 5 nM Pomalidomide (HY-10984) synergistically reduces the viability of IMiD-resistant t (4;14) H929-POMR multiple myeloma cells by more than 33%[1].
Combination treatment with Gintemetostat (500 nM; 24 h) and 0.1 nM Mezigdomide (HY-129395) synergistically reduces the viability of IMiD-resistant t (4;14) H929-POMR multiple myeloma cells by more than 90%[1].
Gintemetostat (0.5 μM; 24 h) enhances Teclistamab (HY-P99392)-mediated lysis of t (4;14) XG26 multiple myeloma cells (resulting in a 52% cell lysis rate) and promotes the activation of early CD4+ and CD8+ T cells[1].
Combination treatment with Gintemetostat (1 μM; 24 h) and 0.1 μg/mL Talquetamab (HY-P99394) mildly enhances Talquetamab-mediated lysis of t (4;14) XG26 multiple myeloma cells, potentiates Talquetamab-induced lysis of non-t (4;14), high NSD2-expressing XG12 multiple myeloma cells, and induces mild early activation of CD4+ and CD8+ T cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:IMiD-resistant t(4;14) myeloma H929-POMR cells
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Concentration:0.5 μM、1 μM、2.5 μM
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Incubation Time:/
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Result:Combining with 5 nM Pomalidomide synergistically reduced the viability of IMiD-resistant t(4;14) myeloma H929-POMR cells.
The cell viability of 5 nM Pomalidomide alone was 84%, while the combined concentrations decreased to 57%, 38%, and 33%, respectively.
Chemical Information
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No. CAS 2604513-16-6
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Appearance Solid
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Peso molecular 546.52
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Fòrmula C25H26F4N8O2
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Color White to off-white
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SMILES
FC(C=C(C(F)=C1)OC)=C1C2=NC=C(N3C[C@](N)(CCC3)[C@H](O)C(F)F)C(CN4C5=NC=NC(N)=C5N=C4)=C2
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Synonyms
KTX-1001
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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bioRxiv
Spatially-Resolved Multiomic Atlas of Leiomyosarcoma Identifies Two Clinically Relevant Epigenetically-Driven Cell States. [Abstract]2026 May 26:2026.05.22.726988. PMID: 42244620
Solvente y solubilidad
DMSO : 100 mg/mL (182.98 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. 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. 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)
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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.57 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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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.
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
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Ficha de datos (283 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[4]. Lewis CA, et al. Characterization of the activity of KTX-1001, a small molecule inhibitor of multiple myeloma SET domain using surface plasmon resonance. J Biol Chem. 2025;301(7):110382. [Content Brief]
[5]. Ma Z, et al. Drug Discovery Targeting Nuclear Receptor Binding SET Domain Protein 2 (NSD2). J Med Chem. 2023;66(16):10991-11026. [Content Brief]
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. 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 | 1.8298 mL | 9.1488 mL | 18.2976 mL | 45.7440 mL |
| 5 mM | 0.3660 mL | 1.8298 mL | 3.6595 mL | 9.1488 mL | |
| 10 mM | 0.1830 mL | 0.9149 mL | 1.8298 mL | 4.5744 mL | |
| 15 mM | 0.1220 mL | 0.6099 mL | 1.2198 mL | 3.0496 mL | |
| 20 mM | 0.0915 mL | 0.4574 mL | 0.9149 mL | 2.2872 mL | |
| 25 mM | 0.0732 mL | 0.3660 mL | 0.7319 mL | 1.8298 mL | |
| 30 mM | 0.0610 mL | 0.3050 mL | 0.6099 mL | 1.5248 mL | |
| 40 mM | 0.0457 mL | 0.2287 mL | 0.4574 mL | 1.1436 mL | |
| 50 mM | 0.0366 mL | 0.1830 mL | 0.3660 mL | 0.9149 mL | |
| 60 mM | 0.0305 mL | 0.1525 mL | 0.3050 mL | 0.7624 mL | |
| 80 mM | 0.0229 mL | 0.1144 mL | 0.2287 mL | 0.5718 mL | |
| 100 mM | 0.0183 mL | 0.0915 mL | 0.1830 mL | 0.4574 mL |
Gintemetostat Related Classifications
HY-154812 Related Classifications
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- Gintemetostat
- 2604513-16-6
- KTX-1001
- KTX1001
- KTX 1001
- Histone Methyltransferase
- CD44
- XG26 multiple myeloma cells
- H3K36me2
- H929-POMR multiple myeloma cells
- KMS11 multiple myeloma cells
- multiple myeloma
- NSD2/MMSET histone methyltransferase
- XG12 multiple myeloma cells
- T-cell
- relapsed and refractory multiple myeloma
- NSD2 SET domain
- Inhibitor
- inhibitor
- inhibit