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Icovamenib  (Synonyms: BMF-219; Menin-MLL inhibitor 21)

Cat. No.: HY-150105 Pureté: 98.96%
Instruction de manipulation Technical Support

Icovamenib (BMF-219) is a selective, orally active, irreversible Menin inhibitor. Icovamenib forms a stable and irreversible covalent bond with Menin. Icovamenib promotes selective and controlled proliferation of beta cells and improvement of beta cell function in ex vivo human islet cultures. Icovamenib enhances glycemic control in animal diabetic models. Icovamenib induces a dose-dependent enhancement in insulin secretion potentiated by the GLP-1 RA. Icovamenib can be used for the study of multiple hematologic malignancies, solid tumors, and diabetes mellitus, such as diffuse large B-cell lymphoma (DLBCL), multiple myeloma (MM) and chronic lymphocytic leukemia and type 2 diabetes.

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Icovamenib

Icovamenib Chemical Structure

CAS No. : 2448172-22-1

Size Prix Stock Quantité
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
En stock
Solution
10 mM * 1 mL in DMSO En stock
Solid
5 mg En stock
10 mg En stock
25 mg En stock
50 mg En stock
100 mg En stock
200 mg   Obtenir un devis  
500 mg   Obtenir un devis  

* Veuillez sélectionner la quantité avant d'ajouter des articles.

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Description

Icovamenib (BMF-219) is a selective, orally active, irreversible Menin inhibitor. Icovamenib forms a stable and irreversible covalent bond with Menin. Icovamenib promotes selective and controlled proliferation of beta cells and improvement of beta cell function in ex vivo human islet cultures. Icovamenib enhances glycemic control in animal diabetic models. Icovamenib induces a dose-dependent enhancement in insulin secretion potentiated by the GLP-1 RA. Icovamenib can be used for the study of multiple hematologic malignancies, solid tumors, and diabetes mellitus, such as diffuse large B-cell lymphoma (DLBCL), multiple myeloma (MM) and chronic lymphocytic leukemia and type 2 diabetes[1][2][3][4][5].

In Vitro

Icovamenib promotes selective and controlled proliferation of beta cells and improvement of beta cell function in ex vivo human islet cultures, in a concentration- and glucose-dependent manner[2].
Icovamenib shows potent cytotoxicity on various menin-dependent acute myeloid leukemia (AML) cells[3].

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

In Vivo

Icovamenib enhances glycemic control in animal diabetic models[2].

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

Essai clinique
Masse moléculaire

566.65

Formule

C31H34N8O3

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=CC(CN2C[C@@H](CCC2)NC(C=C)=O)=CC=N1)NC3=CC=C(C=C3)C4=CC5=C(N6CCOCC6)N=CN=C5N4

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvant et solubilité
In Vitro: 

DMSO : 25 mg/mL (44.12 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 1.7648 mL 8.8238 mL 17.6476 mL
5 mM 0.3530 mL 1.7648 mL 3.5295 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.

  • Calculateur de molarité

  • Calculateur de dilution

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:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  PBS

    Solubility: 8.33 mg/mL (14.70 mM); Clear solution; Need ultrasonic and adjust pH to 2 with 1 M HCl

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
Pureté et documentation
Références

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 1.7648 mL 8.8238 mL 17.6476 mL 44.1189 mL
5 mM 0.3530 mL 1.7648 mL 3.5295 mL 8.8238 mL
10 mM 0.1765 mL 0.8824 mL 1.7648 mL 4.4119 mL
15 mM 0.1177 mL 0.5883 mL 1.1765 mL 2.9413 mL
20 mM 0.0882 mL 0.4412 mL 0.8824 mL 2.2059 mL
25 mM 0.0706 mL 0.3530 mL 0.7059 mL 1.7648 mL
30 mM 0.0588 mL 0.2941 mL 0.5883 mL 1.4706 mL
40 mM 0.0441 mL 0.2206 mL 0.4412 mL 1.1030 mL
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  • 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.

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Nom du produit:
Icovamenib
Cat. No.:
HY-150105
Quantité:
MCE Japan Authorized Agent: