2. Epigenetics Apoptosis
  3. Epigenetic Reader Domain Apoptosis
  4. Bleximenib

Bleximenib  (Synonyms: JNJ-75276617; Menin-MLL inhibitor 24)

Cat. No.: HY-148669
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Bleximenib (JNJ-75276617; Menin-MLL inhibitor 24) is a potent, selective and orally active menin-KMT2A protein-protein interaction inhibitor with IC50 values of 0.1, 0.045, ≤0.066 nM for human, mouse, dog, respectively. Bleximenib shows antiproliferative activity and induces apoptosis. Bleximenib has the potential for the research of Acute myeloid leukemia (AML).

For research use only. We do not sell to patients.

Bleximenib Chemical Structure

Bleximenib Chemical Structure

CAS No. : 2654081-35-1

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Based on 1 publication(s) in Google Scholar

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Bleximenib Related Antibodies

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  • Purity & Documentation

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Description

Bleximenib (JNJ-75276617; Menin-MLL inhibitor 24) is a potent, selective and orally active menin-KMT2A protein-protein interaction inhibitor with IC50 values of 0.1, 0.045, ≤0.066 nM for human, mouse, dog, respectively. Bleximenib shows antiproliferative activity and induces apoptosis. Bleximenib has the potential for the research of Acute myeloid leukemia (AML)[1][2].

In Vitro

Bleximenib (0-3 µM; 48, 72 h) decreases the gene expression of MEIS1, PBX3, FLT3 in MOLM-14, OCI-AML3 cells[1].
Bleximenib (0-15 µM; 8 days) shows antiproliferative activity[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Bleximenib Related Antibodies

Cell Proliferation Assay[1]

Cell Line: MOLM-14, MOLM-13, MV4-11, THP-1, EOL-1, OCI-AML3, RS4:11, KO-52, HL-60, K562 cells
Concentration: 0-15 µM
Incubation Time: 8 days
Result: Showed antiproliferative activity with IC50s of 0.036, 0.023 0.0054, >15, 0.116, 0.045, 0.040, >10, >15, >15 µM for MOLM-14, MOLM-13, MV4-11, THP-1, EOL-1, OCI-AML3, RS4:11, KO-52, HL-60, K562 cells, respectively.

RT-PCR[1]

Cell Line: MOLM-14, OCI-AML3 cells
Concentration: 0, 4, 12, 37, 111, 333, 1000, 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.

Apoptosis Analysis[1]

Cell Line: MOLM-14, OCI-AML3 AML, RS4;11 B-ALL cells
Concentration: 0, 0.0156, 0.0625, 0.25, 1, 4 µM
Incubation Time: 7 days
Result: Induced apoptosis in a dose-dependent manner.
In Vivo

Bleximenib (30, 50, 100 mg/kg; PO; daily for 5 weeks) shows antitumor activity[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 6- to 8-week-old immune-compromised mice (MOLM-14 AML)[1]
Dosage: 30, 50, 100 mg/kg
Administration: PO; daily for 5 weeks
Result: Induced tumor regressions of 70%, 97%, and 99% at 30, 50, and 100 mg/kg, respectively.
Molecular Weight

599.78

Formula

C32H50FN7O3
CAS No.
Appearance

Oil

Color

Colorless to light yellow

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6673 mL 8.3364 mL 16.6728 mL
5 mM 0.3335 mL 1.6673 mL 3.3346 mL
View the 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.

* 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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C2

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V2

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 99.36%

SDS (252 KB)

COA (255 KB) HNMR (445 KB) RP-HPLC (270 KB) LCMS (97 KB)

Handling Instructions (2659 KB)
References

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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Bleximenib Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Bleximenib2654081-35-1JNJ-75276617 Menin-MLL inhibitor 24JNJ75276617JNJ 75276617Epigenetic Reader DomainApoptosisantiproliferativeapoptosisAcute myeloid leukemiaMOLM-14OCI-AML3anticancerInhibitorinhibitorinhibit

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