Ziftomenib (Synonyms: KO-539) |
Catalog No.GC64518
One-Click Copy Product Info
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Ziftomenib is a highly selective and orally active inhibitor of the Menin-MLL (mixed lineage leukemia) interaction used to treat relapsed or refractory acute myeloid leukemia (AML).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2134675-36-6
Sample solution is provided at 25 µL, 10mM.
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Ziftomenib is a highly selective and orally active inhibitor of the Menin-MLL (mixed lineage leukemia) interaction used to treat relapsed or refractory acute myeloid leukemia (AML)[1, 2]. Ziftomenib can inhibit the proliferation and survival of MLL-rearranged leukemia cells by blocking the binding of Menin protein to MLL fusion protein[3].
In vitro, Ziftomenib (150nM) treatment of AML cell lines (OCI-AML3, MOLM13, MV411 cells) induced transcriptional downregulation of MEIS1, PBX3, FLT3 and BCL2[4].
In vivo, oral treatment of AML cell xenograft mice with Ziftomenib (75mg/kg) significantly reduced the tumor burden in mice and prolonged the survival of mice[5].
References:
[1] Zhao J, Dong X, Che J. Ziftomenib (KO-539): a potent and selective Menin inhibitor for the treatment of recurrent or refractory acute myeloid leukemia[M]//Drug Discovery Stories. Elsevier, 2025: 455-466.
[2] Wang E S, Issa G C, Erba H P, et al. Ziftomenib in relapsed or refractory acute myeloid leukaemia (KOMET-001): A multicentre, open-label, multi-cohort, phase 1 trial[J]. The Lancet Oncology, 2024, 25(10): 1310-1324.
[3] Dhiman S, Dhillon V, Balasubramanian S K. Targeting Menin in Acute Myeloid Leukemia: Therapeutic Advances and Future Directions[J]. Cancers, 2024, 16(22): 3743.
[4] Rausch J, Dzama M M, Dolgikh N, et al. Menin inhibitor ziftomenib (KO-539) synergizes with drugs targeting chromatin regulation or apoptosis and sensitizes acute myeloid leukemia with MLL rearrangement or NPM1 mutation to venetoclax[J]. Haematologica, 2023, 108(10): 2837.
[5] Fiskus W, Daver N, Boettcher S, et al. Activity of menin inhibitor ziftomenib (KO-539) as monotherapy or in combinations against AML cells with MLL1 rearrangement or mutant NPM1[J]. Leukemia, 2022, 36(11): 2729-2733.
| Cell experiment [1]: | |
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Cell lines |
Acute myeloid leukemia (AML) cells (OCI-AML3, MOLM13 and MV411 cells) |
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Preparation Method |
OCI-AML3, MOLM13 and MV411 cells were incubated with 150nM Ziftomenib for 3-4 days, followed by RNA sequencing. |
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Reaction Conditions |
150nM; 3-4 days |
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Applications |
Ziftomenib uniformly induced transcriptional downregulation of MEIS1, PBX3, FLT3, and BCL2 in all NPM1mut (OCI-AML3 cells) and MLL-r cells (MOLM13 and MV411 cells) and demonstrated high consistency with the effects of other menin inhibitors. |
| Animal experiment [2]: | |
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Animal models |
NSG mice |
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Preparation Method |
NSG mice were engrafted with luciferized patient-derived MLL-AF9+FLT3-TKD expressing Acute myeloid leukemia (AML) cells and monitored for 5-7 days. Mice were imaged by Xenogen camera, randomized to equivalent bioluminescence and treated with vehicle, 75mg/kg of Ziftomenib (p.o., daily×5 days) and/or 30mg/kg of OTX015 (p.o., daily×5 days), or 30mg/kg of venetoclax (p.o., daily×5 days) for 2 weeks. Total bioluminescent flux was determined for each cohort by Xenogen camera. |
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Dosage form |
75mg/kg; 5 days; p.o. |
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Applications |
Whereas monotherapy with relatively low dose of venetoclax or OTX015 alone for 2 weeks Exhibited modest reduction of AML burden, treatment with Ziftomenib alone induced marked and significant reduction in AML burden. |
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References: |
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| Cas No. | 2134675-36-6 | SDF | |
| Synonyms | KO-539 | ||
| Formula | C33H42F3N9O2S2 | M.Wt | 717.87 |
| Solubility | Storage | Store at -20°C | |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.393 mL | 6.965 mL | 13.9301 mL |
| 5 mM | 278.6 μL | 1.393 mL | 2.786 mL |
| 10 mM | 139.3 μL | 696.5 μL | 1.393 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)