revumenib

Boiling point: 739.1±70.0°C(Predicted)

Solubility: DMSO: 30.0(Max Conc. mg/mL);47.56(Max Conc. mM)

Form: Solid

Color: White to Off-white

1. Cell Experiment

Solubility in DMSO : ≥ 25 mg/mL (39.63 mM; Hygroscopic DMSO has a significant effect on the solubility of the product, please use freshly opened DMSO)."≥" means soluble, but saturation unknown.

Preparing Stock Solutions：

Please choose the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once it is prepared into a solution, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and duration of the stock solution: -80°C, 1 year; -20°C, 6 months。 Use within 1 year when stored at -80°C, and within 6 months when stored at -20°C.

2. Animal Control

Choose the appropriate dissolution protocol based on your experimental animal and mode of administration.For the following dissolution schemes, please prepare the clarified stock solution according to the in vitro method, and then add the co-solvent in turn:

- In order to ensure the reliability of the experimental results, the clarified stock solution can be properly stored according to the storage conditions; It is recommended that you use the working solution for in vivo experiments and use it on the same day;The percentages shown before the following solvents are the proportion of the volume of that solvent in your final solution; If precipitation and precipitation occur during the preparation process, it can be dissolved by heating and/or ultrasound.

Option 1

Add each solvent in order: 10% DMSO, 40% PEG300, 5% Tween-80, 45% Saline.

Solubility:≥ 4.17 mg/mL (6.61 mM); Clarifying solution

A clarified solution of ≥ 4.17 mg/mL (saturation unknown) is obtained for this protocol.

For example, take 100 μL of 41.7 mg/mL of clarified DMSO stock solution and add it to 400 μL of PEG300 and mix well. Add 50 μL of Tween-80 to the above system and mix well. Then continue to add 450 μL of normal saline to 1 mL.

Preparation of normal saline: 0.9 g of sodium chloride dissolved in ddH₂O and fixed to 100 mL can obtain a clear and transparent normal saline solution.

Option 2

add each solvent in order:10% DMSO;90% (20% SBE-β-CD in Saline)

Solubility: ≥ 4.17 mg/mL (6.61 mM); Clarifying solution

A clarified solution of ≥ 4.17 mg/mL (saturation unknown) is obtained for this protocol.

For example, 100 μL of 41.7 mg/mL of clarified DMSO stock solution is added to 900 μL of 20% SBE-β-CD saline in water and mixed well.

2 g of SBE-β-CD (sulfonbutyl ether β-cyclodextrin) powder is set in 10 mL of normal saline and completely dissolved until clear.

Option 3

add each solvent in order:10% DMSO,90% Corn Oil

Solubility: ≥ 4.17 mg/mL (6.61 mM); Clarifying solution

A clarified solution of ≥ 4.17 mg/mL (saturation unknown) is available for this protocol, as appropriate for animal experiments with experimental cycles of more than half a month.

For example, 100 μL of 41.7 mg/mL of clarified DMSO stock solution was added to 900 μL of corn oil and mixed well.

Option 4

add each solvent in order: 5% DMSO;40% PEG300;5% Tween-80;50% Saline

Solubility: ≥ 2.5 mg/mL (3.96 mM); Clarifying solution

Option 5

add each solvent in order: 5% DMSO;95% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (3.96 mM); Clarifying solution

Option 6

add each solvent in order:1% DMSO;99% Saline

Solubility: ≥ 0.5 mg/mL (0.79 mM); Clarifying solution

Exposure-response relationships for revumenib have not been fully characterized.

Revumenib exhibits a concentration-dependent increase in QTc.Patients at higher risk of QTc prolongation - such as those receiving other QTc-prolonging medications - should use revumenib with caution and should be monitored closely throughout therapy.

Revumenib is an inhibitor of menin, a scaffold protein.Menin interacts with both wild-type and rearranged KMT2A, playing a crucial role in leukemogenesis by activating leukemogenic transcription pathways that drive differentiation arrest and cell proliferation. Revumenib disrupts the interaction between menin and KMT2A, thereby downregulating leukemogenic transcriptional pathways, reversing leukemic differentiation arrest, and promoting maturation of leukemia cells.