Menin-MLL inhibitor-22
Based on 1 Customer Validation
Menin-MLL inhibitor-22 (compound C20) is an orally active inhibitor of the interaction between menin and mixed lineage leukemia (MLL) (IC50=7 nM). Menin-MLL inhibitor-22 binds menin protein and inhibits cancer cell growth (MV4 cells, IC50=0.3 μM). Menin is a putative tumor suppressor associated with multiple endocrine neoplasia type 1 (MEN-1 syndrome).
For research use only. We do not sell to patients.
- Purity: 99.85%
- CAS No.: 2851841-61-5
- Formula: C29H39N7O3S
- Molecular Weight:565.73
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HL-60 | IC50 |
>10 μM
Compound: C20
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Antiproliferative activity against human HL-60 cells harboring MLL-AF4 assessed as cell growth inhibition measured for 72 hrs by MTT assay
Antiproliferative activity against human HL-60 cells harboring MLL-AF4 assessed as cell growth inhibition measured for 72 hrs by MTT assay
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[PMID: 36173787] |
| MV4-11 | IC50 |
0.3 μM
Compound: C20
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Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability measured for 3 days followed by replacement with fresh medium of compound and measured after 72 hrs by cell counting assay
Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability measured for 3 days followed by replacement with fresh medium of compound and measured after 72 hrs by cell counting assay
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[PMID: 36173787] |
| MV4-11 | IC50 |
0.3 μM
Compound: C20
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Antiproliferative activity against human MV4-11 cells harboring MLL-AF4 assessed as cell growth inhibition measured for 72 hrs by MTT assay
Antiproliferative activity against human MV4-11 cells harboring MLL-AF4 assessed as cell growth inhibition measured for 72 hrs by MTT assay
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[PMID: 36173787] |
| MV4-11 | IC50 |
0.3 μM
Compound: 12; C20
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Antiproliferative activity against human MV4-11 cells incubated for 7 days by PrestoBlue Cell Viability assay
Antiproliferative activity against human MV4-11 cells incubated for 7 days by PrestoBlue Cell Viability assay
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[PMID: 38367493] |
| MV4-11 | IC50 |
0.36 μM
Compound: C20
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Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability measured for 3 days by cell counting assay
Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability measured for 3 days by cell counting assay
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[PMID: 36173787] |
Menin-MLL inhibitor-22 (1 μM; 60 min) possesses good stability and low clearance rate in liver microsomes[1].
Menin-MLL inhibitor-22 (1 and 10 μM; 24 h) inhibits MLL-r Leukemia cells MV4;11 growth and (0.1-10 μM; 24 h) decreases the expression of the HOXA9 and MEIS1 induced by menin-MLL interaction[1].
Menin-MLL inhibitor-22 (1, and 10 μM; 7 d) increases the amount of CD11b, a differentiation marker of myeloid cells, indicating a reverse the differentiation arrest of MLL-r leukemia cells[1].
Menin-MLL inhibitor-22 (1, and 10 μM; 24 h) induces cell apoptosis and G0/G1 cell cycle arrest[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MLL-r Leukemia cells MV4;11
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Concentration:0.1, 1, and 10 μM
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Incubation Time:24 hours
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Result:Reversed the over-expressing HOXA9 and MEIS1 induced by menin-MLL interaction, decreased the level of HOXA9 and MEIS1.
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Cell Line:MLL-r Leukemia cells MV4;11
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Concentration:1, and 10 μM
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Incubation Time:24 hours
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Result:Decreased in the population of cells in the S and G2/M phases, arrested cell cycle at G0/G1 phase.
Pharmacokinetic Properties in SD Rats[1]
| Route | Dose (mg/kg) | Tmax (h) | T1/2 (h) | MRT (h) | Cmax (ng/mL) | AUC0-t (ng·h/mL) | AUC0-∞ (ng·h/mL) | Cltotal (mL/h/kg) | Vss (L/kg) | F (%) |
| i.v. | 5 | N/A | 17.5 | 7.1 | 1187 | 1700 | 2495 | 2056 | 49.3 | |
| p.o. | 15 | 7.3 | 15.5 | 12.0 | 56.7 | 863.7 | 1476 | 10730 | 23 | 16.9 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Balb/C nude mice bearing MV4;11 cell xenografts[1]
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Dosage:6 mg/kg, 30 mg/kg
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Administration:Oral gavage; every second day for 16 days
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Result:Reduced the volume of tumor in mice.
Chemical Information
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CAS No. 2851841-61-5
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Appearance Solid
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Molecular Weight 565.73
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Formula C29H39N7O3S
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Color White to off-white
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SMILES
O=S(C1=CC=C(N2CC(CN3CCC(NC4=NC=NC5=CC=C(N=C54)OCCN(C)C)CC3)C2)C=C1)(C6CC6)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 125 mg/mL (220.95 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (273 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7676 mL | 8.8381 mL | 17.6763 mL | 44.1907 mL |
| 5 mM | 0.3535 mL | 1.7676 mL | 3.5353 mL | 8.8381 mL | |
| 10 mM | 0.1768 mL | 0.8838 mL | 1.7676 mL | 4.4191 mL | |
| 15 mM | 0.1178 mL | 0.5892 mL | 1.1784 mL | 2.9460 mL | |
| 20 mM | 0.0884 mL | 0.4419 mL | 0.8838 mL | 2.2095 mL | |
| 25 mM | 0.0707 mL | 0.3535 mL | 0.7071 mL | 1.7676 mL | |
| 30 mM | 0.0589 mL | 0.2946 mL | 0.5892 mL | 1.4730 mL | |
| 40 mM | 0.0442 mL | 0.2210 mL | 0.4419 mL | 1.1048 mL | |
| 50 mM | 0.0354 mL | 0.1768 mL | 0.3535 mL | 0.8838 mL | |
| 60 mM | 0.0295 mL | 0.1473 mL | 0.2946 mL | 0.7365 mL | |
| 80 mM | 0.0221 mL | 0.1105 mL | 0.2210 mL | 0.5524 mL | |
| 100 mM | 0.0177 mL | 0.0884 mL | 0.1768 mL | 0.4419 mL |
Menin-MLL inhibitor-22 Related Classifications
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