Ziftomenib
Based on 2 publication(s) in Google Scholar
Ziftomenib (KO-539) is an orally active menin-MLL interaction inhibitor with antitumor activities (WO2017161028A1, compound 151).
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.43%
- CAS No.: 2134675-36-6
- Formule: C33H42F3N9O2S2
- Masse moléculaire:717.87
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Ziftomenib
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Flow Cytometry
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Cell Proliferation/Viability Assay
Activité biologique
The mixed-lineage leukemia (MLL) protein is a histone methyltransferase critical for the epigenetic regulation of gene transcription. Many acute leukemias, including acute myeloblastic leukemia (AML), acute lymphoblastic leukemia (ALL) and mixed-lineage leukemia (MLL), are characterized by the presence of chimeric MLL fusion proteins that result from chromosomal translocations of the MLL gene located at chromosome 11, band q23 (11q23). MLL fusion proteins lack the original histone methyltransferase activity of the C-terminus of MLL and gain the ability to regulate transcription of numerous oncogenes, including HOX and MEIS1, resulting in increased cell proliferation and decreased cell differentiation, ultimately leading to leukemogenesis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2134675-36-6
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Appearance Solid
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Masse moléculaire 717.87
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Formule C33H42F3N9O2S2
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Color Off-white to light yellow
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SMILES
N#CC(N1C[C@@H](N2CCN(S(=O)(C)=O)CC2)C)=CC3=C1C=CC(CN4CCC(NC5=C(C=C(CC(F)(F)F)S6)C6=NC(NC)=N5)CC4)=C3C
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Synonyms
KO-539
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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Blood
Overcoming menin inhibitor resistance in AML cells with combinations including BET proteins and a dual BRG1/BRM inhibitor. [Abstract]2026 Feb 24:blood.2025031486. PMID: 41734382 -
Leukemia
Causal linkage of presence of mutant NPM1 to efficacy of novel therapeutic agents against AML cells with mutant NPM1. [Abstract]2023 Jun;37(6):1336-1348. PMID: 36977823
Ziftomenib purchased from MedChemExpress. Usage Cited in: Leukemia. 2023 Jun;37(6):1336-1348. [Abstract]
Ziftomenib (10-300 nM; 96 h) induced loss of viability in OCI-AML3 cells with and without mtNPM1 KO.
Ziftomenib purchased from MedChemExpress. Usage Cited in: Leukemia. 2023 Jun;37(6):1336-1348. [Abstract]
Ziftomenib (10-300 nM; 96 h) dose-dependently induced significantly greater loss of viability in OCIAML2 NPM1mtA/wt versus OCI-AML2 NPM1wt/wt cells.
Solvant et solubilité
DMSO : 100 mg/mL (139.30 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Ethanol : 25 mg/mL (34.83 mM; ultrasonic and warming and heat to 60°C)
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)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (2.90 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (273 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)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
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 | 1.3930 mL | 6.9650 mL | 13.9301 mL | 34.8252 mL |
| 5 mM | 0.2786 mL | 1.3930 mL | 2.7860 mL | 6.9650 mL | |
| 10 mM | 0.1393 mL | 0.6965 mL | 1.3930 mL | 3.4825 mL | |
| 15 mM | 0.0929 mL | 0.4643 mL | 0.9287 mL | 2.3217 mL | |
| 20 mM | 0.0697 mL | 0.3483 mL | 0.6965 mL | 1.7413 mL | |
| 25 mM | 0.0557 mL | 0.2786 mL | 0.5572 mL | 1.3930 mL | |
| 30 mM | 0.0464 mL | 0.2322 mL | 0.4643 mL | 1.1608 mL | |
| DMSO | 40 mM | 0.0348 mL | 0.1741 mL | 0.3483 mL | 0.8706 mL |
| 50 mM | 0.0279 mL | 0.1393 mL | 0.2786 mL | 0.6965 mL | |
| 60 mM | 0.0232 mL | 0.1161 mL | 0.2322 mL | 0.5804 mL | |
| 80 mM | 0.0174 mL | 0.0871 mL | 0.1741 mL | 0.4353 mL | |
| 100 mM | 0.0139 mL | 0.0697 mL | 0.1393 mL | 0.3483 mL |
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