Bleximenib
Based on 2 publication(s) in Google Scholar
Bleximenib (JNJ-75276617) is an orally active and selective menin-KMT2A inhibitor, with IC50 values of 0.1 nM, 0.045 nM, and ≤0.066 nM for humans, mice, and dogs, respectively. Bleximenib can inhibit the proliferation and induce apoptosis and differentiation of tumor cells. Bleximenib can be used in the research of tumors such as leukemia.
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- Pureza: 99.24%
- No. CAS: 2654081-35-1
- Fòrmula: C32H50FN7O3
- Peso molecular:599.78
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Almacenamiento:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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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) Bleximenib
MoreVer todos los productos específicos de isoformas Histone Methyltransferase
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Actividad biológica
Bleximenib (0-3 µM; 48-72 h) can reduce the expression of MEIS1, PBX3, FLT3, and JMJD1C in MOLM-14 and OCI-AML3 cells[1].
Bleximenib (0-15 µM; 7-8 days) can inhibit the proliferation of leukemia cells and induce apoptosis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MOLM-14 and OCI-AML3 cells
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Concentration:0, 4, 12, 37, 111, 333, 1000 and 3000 nM
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Incubation Time:MOLM-14 cells for 48 h, OCI-AML3 cells for 72 h
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Result:Decreased the gene expression of MEIS1, PBX3, FLT3, JMJD1C.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female immune-compromised mice aged 6-8 week old treated AML or ALL cells[1]
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Dosage:10, 30, 50 and 100 mg/kg
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Administration:Oral administration (p.o.); 4-6 weeks
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Result:Led to dose-dependent tumor regressions.
Significantly increased the lifespan of mice.
Increased the expression of differentiation markers.
Chemical Information
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No. CAS 2654081-35-1
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Appearance Oil
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Peso molecular 599.78
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Fòrmula C32H50FN7O3
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Color Colorless to light yellow
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SMILES
COCCN(C)CCC[C@@H](N1CC2(C1)CN(C3=NC=NN=C3OC4=C(C=C(C=C4)F)C(N(CC)C(C)C)=O)CC2)C(C)C
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Synonyms
JNJ-75276617; Menin-MLL inhibitor 24
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (2)
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Journal Impact Factor
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Most Recent
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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 -
Nat Commun
CRISPR base editor screening identifies spectrum of MEN1 mutations impacting menin inhibitors in clinical trials. [Abstract]2026 May 9. PMID: 42103719
Solvente y solubilidad
DMSO : 100 mg/mL (166.73 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 100 mg/mL (166.73 mM; Need ultrasonic)
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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.17 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 (4.17 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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Pureza y Documentación
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Ficha de datos (278 KB)
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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)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Kwon MC, et al. Preclinical efficacy of the potent, selective menin-KMT2A inhibitor JNJ-75276617 (bleximenib) in KMT2A- and NPM1-altered leukemias. Blood. 2024 Sep 12;144(11):1206-1220. [Content Brief]
[2]. Hogeling SM, et al. Bleximenib, the novel menin-KMT2A inhibitor JNJ-75276617, impairs long-term proliferation and immune evasion in acute myeloid leukemia. Haematologica. 2024 Dec 19. [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 (protect from 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 / H2O | 1 mM | 1.6673 mL | 8.3364 mL | 16.6728 mL | 41.6819 mL |
| 5 mM | 0.3335 mL | 1.6673 mL | 3.3346 mL | 8.3364 mL | |
| 10 mM | 0.1667 mL | 0.8336 mL | 1.6673 mL | 4.1682 mL | |
| 15 mM | 0.1112 mL | 0.5558 mL | 1.1115 mL | 2.7788 mL | |
| 20 mM | 0.0834 mL | 0.4168 mL | 0.8336 mL | 2.0841 mL | |
| 25 mM | 0.0667 mL | 0.3335 mL | 0.6669 mL | 1.6673 mL | |
| 30 mM | 0.0556 mL | 0.2779 mL | 0.5558 mL | 1.3894 mL | |
| 40 mM | 0.0417 mL | 0.2084 mL | 0.4168 mL | 1.0420 mL | |
| 50 mM | 0.0333 mL | 0.1667 mL | 0.3335 mL | 0.8336 mL | |
| 60 mM | 0.0278 mL | 0.1389 mL | 0.2779 mL | 0.6947 mL | |
| 80 mM | 0.0208 mL | 0.1042 mL | 0.2084 mL | 0.5210 mL | |
| 100 mM | 0.0167 mL | 0.0834 mL | 0.1667 mL | 0.4168 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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