2. Apoptosis Epigenetics Protein Tyrosine Kinase/RTK
  3. Apoptosis Histone Methyltransferase FLT3
  4. Bleximenib

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

Cat. No.: HY-148669
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COA
Handling Instructions Technical Support

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.

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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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Bleximenib:

Bleximenib Related Antibodies

Top Publications Citing Use of Products

View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms
EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1][2].

In Vitro

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.

Bleximenib Related Antibodies

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

Bleximenib (0-100 mg/kg; orally administered; 4-6 weeks) exhibits anti-tumor activity in mouse models of leukemia[1].

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

Animal Model: Female immune-compromised mice aged 6-8 week old treated AML or ALL cells[1]
Dosage: 10, 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.
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)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

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 75276617ApoptosisHistone MethyltransferaseFLT3Cluster of differentiation antigen 135CD135Fms like tyrosine kinase 3leukemia modelALL. AMLInhibitorinhibitorinhibit

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