Menin-MLL-IN-37
Menin-MLL-IN-37 is an orally active Menin-MLL protein complex inhibitor with an IC50 of 820.50 nM. Menin-MLL-IN-37 disrupts the interaction between menin and MLL proteins. Menin-MLL-IN-37 induces differentiation of acute myeloid leukemia cells and selectively inhibits the proliferation of MLL-rearranged and DNMT3A/NPM1-mutant leukemia cells. Menin-MLL-IN-37 can be used for the research of acute myeloid leukemia (AML).
For research use only. We do not sell to patients.
- Formula: C29H37F3N6O3S2
- Molecular Weight:638.77
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
Menin-MLL 820.50 nM (IC50) |
In Vitro
Menin-MLL-IN-37 (Compound A13) potently inhibits the proliferation of MLL-rearranged (MV4-11, MOLM-13), DNMT3A/NPM1-mutated (OCI-AML3) and other leukemia cell lines (THP-1, HL-60, K562), with IC50 values of 0.379, 0.838, 0.763, 1.618, 1.179 and 2.653 μM[1].
Menin-MLL-IN-37 (1-2 μM; 7 days) induces differentiation of MV4-11 and MOLM-13 leukemia cells, resulting in increased surface expression levels of CD11b[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:MV4-11, MOLM-13 leukemia cell lines
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Concentration:1000 nM, 2000 nM
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Incubation Time:7 days
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Result:Induced a significant increase in the percentage of CD11b-positive cells in MV4-11 cell line.
Induced a significant increase in the percentage of CD11b-positive cells in MOLM-13 cell line.
Parmacokinetics
| Species | Dose | Route | Tmax | T1/2 | Cmax | AUC0-t | AUC0-∞ | MRT0-t | Vz/F | CL/F |
|---|---|---|---|---|---|---|---|---|---|---|
| Mice[1] | 20 mg/kg | i.g. | 1.67 h | 2.43 h | 537.00 ng/mL | 2241.09 ng·h/mL | 2379.51 ng·h/mL | 3.59 h | 30499.24 mL/kg | 147.32 mL/min/kg |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Molecular Weight 638.77
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Formula C29H37F3N6O3S2
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SMILES
FC(F)(F)CC1=CC2=C(NC3CCN(CC4CCN(C5=CC=C(S(=O)(N6CCOCC6)=O)C=C5)CC4)CC3)N=CN=C2S1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Immunoprecipitation
Immunoprecipitation (IP) is an experimental method that uses the principle of antibody specific binding to purify and enrich target proteins.
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Co-Immunoprecipitation
Co-immunoprecipitation technology can verify protein interaction based on the specific immune reaction between antibodies and antigens.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)