| Field | Specification |
|---|---|
| Alternative names | JNJ-75276617 oxalate; Menin-MLL inhibitor 24 oxalate |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C34H52FN7O7 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Bleximenib oxalate, also known as JNJ-75276617 oxalate and Menin-MLL inhibitor 24 oxalate, is an orally active, selective inhibitor of menin-KMT2A, with IC50 values of 0.1 nM, 0.045 nM and ≤0.066 nM in human, mouse and dog systems, respectively. It can inhibit proliferation and induce apoptosis and differentiation of tumor cells, and can be used in research on tumors such as leukemia[1][2]. It is supplied as an off-white to light yellow solid (C34H52FN7O7, MW 689.82) at 98.0% purity.
Physical & Chemical Properties
| CAS Number | 2866179-95-3 |
|---|---|
| Molecular Formula | C34H52FN7O7 |
| Molecular Weight | 689.82 g/mol |
| Purity | 98.0% |
| Appearance | Solid |
| Color | Off-white to light yellow |
| 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 |
| Signaling Pathway | Apoptosis; Epigenetics; Protein Tyrosine Kinase/RTK |
| Solubility | In Vitro: DMSO: 100 mg/mL (144.97 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) H2O: 50 mg/mL (72.48 mM; Requires sonication) |
| Storage | Powder: -20°C, 3 years. In solvent: -80°C, 6 months; -20°C, 1 month. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 100 mg/mL (144.97 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
| H2O | 50 mg/mL (72.48 mM) | requires sonication |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); avoid repeated freeze-thaw cycles.
If water is used as the stock solvent, dilute to the working solution and sterilize it through a 0.22 μm filter before use.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 2.5 mg/mL (3.62 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 2.5 mg/mL (3.62 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Protocol 3
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 2.5 mg/mL (3.62 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
In MOLM-14 and OCI-AML3 cells, Bleximenib (0-3 μM; 48-72 h) oxalate can lower MEIS1, PBX3, FLT3, and JMJD1C expression[1]. Bleximenib (0-15 μM; 7-8 days) oxalate can suppress leukemia cell proliferation and induce apoptosis[1].
Real Time qPCR[1]
| Cell Line | MOLM-14 and OCI-AML3 cells |
|---|---|
| Concentration | 0, 4, 12, 37, 111, 333, 1000 and 3000 nM |
| Incubation Time | MOLM-14 cells for 48 h, OCI-AML3 cells for 72 h |
| Result | Decreased the gene expression of MEIS1, PBX3, FLT3, JMJD1C. |
In Vivo
In mouse models of leukemia, Bleximenib (0-100 mg/kg; orally administered; 4-6 weeks) oxalate shows anti-tumor activity[1].
| Animal Model | Female immune-compromised mice aged 6-8 week old treated AML or ALL cells[1] |
|---|---|
| Dosage | 0, 30, 50 and 100 mg/kg |
| Administration | Oral administration (p.o.); 4-6 weeks |
| Result | Led to dose-dependent tumor regressions. Significantly increased the lifespan of mice. Increased the expression of differentiation markers. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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Overcoming menin inhibitor resistance in AML cells with combinations including BET proteins and a dual BRG1/BRM inhibitor. Blood 2026 Feb 24:blood.2025031486. PMID: 41734382
CRISPR base editor screening identifies spectrum of MEN1 mutations impacting menin inhibitors in clinical trials. Nat Commun 2026 May 9. PMID: 42103719