Bleximenib oxalate
Based on 2 publication(s) in Google Scholar
Bleximenib (JNJ-75276617) oxalate 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 oxalate can inhibit the proliferation and induce apoptosis and differentiation of tumor cells. Bleximenib oxalate can be used in the research of tumors such as leukemia.
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- Pureza: 98.0%
- No. CAS: 2866179-95-3
- Fòrmula: C34H52FN7O7
- Peso molecular:689.82
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Almacenamiento:Powder -20°C, 3 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
Publications Citing Use of MedChemExpress (MCE) Bleximenib oxalate
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Actividad biológica
Descripciòn
In Vitro
Bleximenib (0-3 µM; 48-72 h) oxalate 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) oxalate 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.
In Vivo
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:0, 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.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 2866179-95-3
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Appearance Solid
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Peso molecular 689.82
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Fòrmula C34H52FN7O7
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Color Off-white to light yellow
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SMILES
O=C(O)C(O)=O.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 oxalate; Menin-MLL inhibitor 24 oxalate
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
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
In Vitro:
DMSO : 100 mg/mL (144.97 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 50 mg/mL (72.48 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. 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. 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)
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 (3.62 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 (3.62 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.
In Vivo Dissolution Calculator
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 (276 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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. 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 |
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| H2O / DMSO | 1 mM | 1.4497 mL | 7.2483 mL | 14.4965 mL | 36.2413 mL |
| 5 mM | 0.2899 mL | 1.4497 mL | 2.8993 mL | 7.2483 mL | |
| 10 mM | 0.1450 mL | 0.7248 mL | 1.4497 mL | 3.6241 mL | |
| 15 mM | 0.0966 mL | 0.4832 mL | 0.9664 mL | 2.4161 mL | |
| 20 mM | 0.0725 mL | 0.3624 mL | 0.7248 mL | 1.8121 mL | |
| 25 mM | 0.0580 mL | 0.2899 mL | 0.5799 mL | 1.4497 mL | |
| 30 mM | 0.0483 mL | 0.2416 mL | 0.4832 mL | 1.2080 mL | |
| 40 mM | 0.0362 mL | 0.1812 mL | 0.3624 mL | 0.9060 mL | |
| 50 mM | 0.0290 mL | 0.1450 mL | 0.2899 mL | 0.7248 mL | |
| 60 mM | 0.0242 mL | 0.1208 mL | 0.2416 mL | 0.6040 mL | |
| DMSO | 80 mM | 0.0181 mL | 0.0906 mL | 0.1812 mL | 0.4530 mL |
| 100 mM | 0.0145 mL | 0.0725 mL | 0.1450 mL | 0.3624 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.
Bleximenib oxalate Related Classifications
HY-148669A Related Classifications
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