MM927
Based on 1 Customer Validation
MM927 is a potent NVL inhibitor, with an IC50 of 0.053 μM. MM927 blocks 60S ribosomal subunit biogenesis in the nucleolus. MM927 induces half-mer polysomes, cell cycle arrest at G1/S and G2/M and apoptosis in cells. MM927 demonstrates antitumor efficacy in MOLM-13 AML and HCT116 CRC xenograft models. MM927 can be used for the study of cancers such as acute myeloid leukemia (AML) and colorectal cancer (CRC).
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- Purity: 99.17%
- CAS No.: 3065567-21-4
- 화학식: C26H18FN3O4S
- 분자량:487.50
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보관:Powder -20°C, 3 years , 4°C, 2 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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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
MM927 (72 h) inhibits viability of HCT116 cells (IC50 = 53 nM) and MOLM-13 cells (IC50 = 92 nM)[1].
MM927 (0.5 μM, 24 h) induces half-mer polysomes and reduces free 60S/80S peaks in polysome profiles of HCT116 NVL WT cells[1].
MM927 (3 μM, 6 h) shifts newly synthesized eL36-SNAP (60S subunit marker) to non-ribosomal fractions and depletes it from 60S/80S/polysome fractions in HCT116 cells[1].
MM927 (3 μM, 24 h) causes reduction in cytoplasmic signal of newly synthesized eL36-SNAP (60S) and retains it in nucleolar foci (colocalized with Fibrillarin) in HCT116 NVL WT cells[1].
MM927 (0.5 μM, 24-48 h) induces G1/S and G2/M cell cycle arrest in HCT116 mock cells[1].
MM927 (3 μM, 2-3 days) triggers apoptosis in MOLM-13 cells, as shown by decreased procaspase-3 and increased cleaved caspase-3 levels, and high Annexin V-positive cell rates[1].
MM927 (0.051 μM, 72 h) inhibits the viability of HCT116 NVLAID/AID cells expressing ectopic human NVL with an IC50 of 0.051 μM, and inhibits HCT116 NVLAID/AID cells expressing ectopic mouse NVL with an IC50 of 0.207 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MOLM-13 cells
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Concentration:3 μM
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Incubation Time:2, 3 days
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Result:Induced apoptosis in MOLM-13 cells.
Decreased procaspase-3.
Increased cleaved caspase-3 levels, and high Annexin V-positive cell rates.
MM927 (35 mg/kg, i.p., twice daily, 14 days) causes reduction in leukemic disease burden in NSG mice[1].
MM927 (35 mg/kg, i.p., twice daily, 3 days) increases nuclear p53 staining and reduces Ki-67-positive cell staining in HCT116 NVL WT tumor xenografts of NSG mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:HCT116 NVL WT cells or HCT116 NVL R403WCRISPR cells (5 × 106 in 100 µL) were subcutaneously implanted into the left and right flanks of 4-8-week-old NSG mice[1]
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Dosage:35 mg/kg
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Administration:i.p., twice daily, 21 days
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Result:Achieved tumor growth inhibition (TGI) in HCT116 NVL WT tumor xenografts of NSG mice.
Reduced tumor burden at the end of treatment.
Showed no effect on HCT116 NVL R403WCRISPR tumor xenografts.
Showed no significant changes in body weight, no significant alterations in hemoglobin, platelets, liver Enzymes (ALT, AST).
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Animal Model:Luciferase-expressing MOLM-13 cells (1 × 106) were intravenously injected into the tail vein of 4-8-week-old NSG mice[1]
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Dosage:35 mg/kg
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Administration:i.p., twice daily, 14 days
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Result:Achieved a 7-fold reduction in leukemic disease burden.
Caused a 9-fold decrease in MOLM-13 cell percentage in bone marrow and a 15-fold decrease in peripheral blood.
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Animal Model:HCT116 NVL WT cells or HCT116 NVL R403WCRISPR cells (5 × 106 in 100 µL) were subcutaneously implanted into the left and right flanks of 4-8-week-old NSG mice[1]
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Dosage:35 mg/kg
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Administration:i.p., twice daily, 3 days
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Result:Reduced Ki-67-positive (proliferating) cell staining in HCT116 NVL WT tumor xenografts of NSG mice, with few cells showing co-localization of p53 and Ki-67.
Chemical Information
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CAS No. 3065567-21-4
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Appearance Solid
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분자량 487.50
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화학식 C26H18FN3O4S
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Color White to off-white
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SMILES
O=C1OC2=CC=C(C(NC3=CC=C4C(SC5=CC(F)=CC=C5C(N4CC#CC)=O)=C3)=O)C=C2N1C
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 25 mg/mL (51.28 mM; ultrasonic and warming and heat to 60°C; 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)
순도&문서
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Data Sheet (279 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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 | 2.0513 mL | 10.2564 mL | 20.5128 mL | 51.2821 mL |
| 5 mM | 0.4103 mL | 2.0513 mL | 4.1026 mL | 10.2564 mL | |
| 10 mM | 0.2051 mL | 1.0256 mL | 2.0513 mL | 5.1282 mL | |
| 15 mM | 0.1368 mL | 0.6838 mL | 1.3675 mL | 3.4188 mL | |
| 20 mM | 0.1026 mL | 0.5128 mL | 1.0256 mL | 2.5641 mL | |
| 25 mM | 0.0821 mL | 0.4103 mL | 0.8205 mL | 2.0513 mL | |
| 30 mM | 0.0684 mL | 0.3419 mL | 0.6838 mL | 1.7094 mL | |
| 40 mM | 0.0513 mL | 0.2564 mL | 0.5128 mL | 1.2821 mL | |
| 50 mM | 0.0410 mL | 0.2051 mL | 0.4103 mL | 1.0256 mL |
MM927 Related Classifications
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