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

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

Cat. No.: HY-148669A Pureza: 98.97%
COA
SDS
Instrucciones de manejo Technical Support

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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Bleximenib oxalate

Bleximenib oxalate Estructura química

No. CAS : 2866179-95-3

Tamaño Precio Stock Cantidad
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 En stock
Solution
10 mM * 1 mL in DMSO En stock
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Based on 1 publication(s) in Google Scholar

Other Forms of Bleximenib oxalate:

Bleximenib oxalate Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Bleximenib oxalate

Ver todos los productos específicos de isoformas Histone Methyltransferase:

Ver todas las isoformas
EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 NSD3/WHSC1L1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

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Descripciòn

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[1][2].

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.

Bleximenib oxalate 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) oxalate 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: 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.
Ensayo clínico
Peso molecular

689.82

Fòrmula

C34H52FN7O7
No. CAS
Appearance

Solid

Color

Light yellow to 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
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.4497 mL 7.2483 mL 14.4965 mL
5 mM 0.2899 mL 1.4497 mL 2.8993 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Calculadora de molaridad

  • Calculadora de dilución

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 (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.
  • Protocol 2

    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:

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.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación

Purity: 98.97%

SDS (252 KB)

COA (252 KB) HNMR (104 KB) RP-HPLC (172 KB) NP-HPLC (125 KB) LCMS (106 KB)

Instrucciones de manejo (2659 KB)
Referencias

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
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
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
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Bleximenib oxalate 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:

Bleximenib2866179-95-3JNJ-75276617Menin-MLL inhibitor 24JNJ75276617JNJ 75276617ApoptosisHistone MethyltransferaseFLT3Cluster of differentiation antigen 135CD135Fms like tyrosine kinase 3CancerleukemiaMeninMLLInhibitorinhibitorinhibit

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Bleximenib oxalate
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