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Balomenib (ZE63-0302) is an orally bioavailable menin-KMT2A interaction inhibitor. Balomenib disrupts menin-KMT2A binding, reverses aberrant HOX gene expression. Balomenib inhibits Meis1 mRNA expression in KMT2A-rearranged acute myeloid leukemia cells. Balomenib can be used for the research of leukemia.

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

Balomenib

Balomenib Chemical Structure

CAS No. : 2939850-17-4

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Based on 1 publication(s) in Google Scholar

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Description

Balomenib (ZE63-0302) is an orally bioavailable menin-KMT2A interaction inhibitor. Balomenib disrupts menin-KMT2A binding, reverses aberrant HOX gene expression. Balomenib inhibits Meis1 mRNA expression in KMT2A-rearranged acute myeloid leukemia cells. Balomenib can be used for the research of leukemia[1].

In Vitro

Balomenib inhibits Meis1 mRNA expression in MOLM‑13 cells (KMT2Ar/MLLr AML cell line) in an exposure‑dependent manner, with peak inhibition at Cmax in an ex vivo plasma inhibitory assay (PIA)[1].
Balomenib disrupts the binding of menin to KMT2A to reverse aberrant HOX gene overexpression driven by menin‑KMT2A interaction in KMT2Ar and NPM1c mutant AML cells[1].

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

Molecular Weight

617.66

Formula

C33H34F3N7O2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

FC(F)(F)CC1=CC(C(N(C2)CC2(CC3)CCN3CC4=CC=C(N(C(C#N)=C5)C[C@@H]6CNC(CO6)=O)C5=C4C)=NC=N7)=C7C=C1

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Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (161.90 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 2.44 mg/mL (3.95 mM; ultrasonic and adjust pH to 3 with 1 M HCl)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6190 mL 8.0951 mL 16.1901 mL
5 mM 0.3238 mL 1.6190 mL 3.2380 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.

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Purity & Documentation
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. 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
Ethanol / DMSO 1 mM 1.6190 mL 8.0951 mL 16.1901 mL 40.4753 mL
DMSO 5 mM 0.3238 mL 1.6190 mL 3.2380 mL 8.0951 mL
10 mM 0.1619 mL 0.8095 mL 1.6190 mL 4.0475 mL
15 mM 0.1079 mL 0.5397 mL 1.0793 mL 2.6984 mL
20 mM 0.0810 mL 0.4048 mL 0.8095 mL 2.0238 mL
25 mM 0.0648 mL 0.3238 mL 0.6476 mL 1.6190 mL
30 mM 0.0540 mL 0.2698 mL 0.5397 mL 1.3492 mL
40 mM 0.0405 mL 0.2024 mL 0.4048 mL 1.0119 mL
50 mM 0.0324 mL 0.1619 mL 0.3238 mL 0.8095 mL
60 mM 0.0270 mL 0.1349 mL 0.2698 mL 0.6746 mL
80 mM 0.0202 mL 0.1012 mL 0.2024 mL 0.5059 mL
100 mM 0.0162 mL 0.0810 mL 0.1619 mL 0.4048 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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Balomenib
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HY-172416
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