WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H414734
CAS#: 2134675-36-6
Description: Ziftomenib, also known as KO539, is an orally bioavailable inhibitor of the menin-mixed lineage leukemia (MLL; myeloid/lymphoid leukemia; KMT2A) fusion protein, with potential antineoplastic activity. Upon oral administration, ziftomenib prevents the interaction between the two proteins menin and MLL, and thus the formation of the menin-MLL complex. This reduces the expression of downstream target genes and results in an inhibition of the proliferation of MLL-rearranged leukemic cells. The menin-MLL complex plays a key role in the survival, growth and proliferation of certain kinds of leukemia cells.
Hodoodo Cat#: H414734
Name: Ziftomenib
CAS#: 2134675-36-6
Chemical Formula: C33H42F3N9O2S2
Exact Mass: 717.29
Molecular Weight: 717.880
Elemental Analysis: C, 55.21; H, 5.90; F, 7.94; N, 17.56; O, 4.46; S, 8.93
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Synonym: Ziftomenib; KO539; KO 539; KO-539;
IUPAC/Chemical Name: (S)-4-Methyl-5-((4-((2-(methylamino)-6-(2,2,2-trifluoroethyl)thieno(2,3-d)pyrimidin-4-yl)amino)piperidin-1-yl)methyl)-1-(2-(4-(methylsulfonyl)piperazin-1-yl)propyl)-1H-indole-2-carbonitrile
InChi Key: BGGALFIXXQOTPY-NRFANRHFSA-N
InChi Code: InChI=1S/C33H42F3N9O2S2/c1-21(43-11-13-44(14-12-43)49(4,46)47)19-45-25(18-37)15-27-22(2)23(5-6-29(27)45)20-42-9-7-24(8-10-42)39-30-28-16-26(17-33(34,35)36)48-31(28)41-32(38-3)40-30/h5-6,15-16,21,24H,7-14,17,19-20H2,1-4H3,(H2,38,39,40,41)/t21-/m0/s1
SMILES Code: 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
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: To be determined
Shelf Life: >2 years if stored properly
Drug Formulation: To be determined
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
| Biological target: | |
| In vitro activity: | |
| In vivo activity: |
The following data is based on the product molecular weight 717.88 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
1: DiNardo KW, LeBlanc TW, Chen H. Novel agents and regimens in acute myeloid leukemia: latest updates from 2022 ASH Annual Meeting. J Hematol Oncol. 2023 Mar 3;16(1):17. doi: 10.1186/s13045-023-01411-x. PMID: 36869366; PMCID: PMC9983204.
2: Fiskus W, Daver N, Boettcher S, Mill CP, Sasaki K, Birdwell CE, Davis JA, Das K, Takahashi K, Kadia TM, DiNardo CD, Burrows F, Loghavi S, Khoury JD, Ebert BL, Bhalla KN. Activity of menin inhibitor ziftomenib (KO-539) as monotherapy or in combinations against AML cells with MLL1 rearrangement or mutant NPM1. Leukemia. 2022 Nov;36(11):2729-2733. doi: 10.1038/s41375-022-01707-w. Epub 2022 Sep 23. PMID: 36151141; PMCID: PMC9613474.
3: Bai H, Zhang SQ, Lei H, Wang F, Ma M, Xin M. Menin-MLL protein-protein interaction inhibitors: a patent review (2014-2021). Expert Opin Ther Pat. 2022 May;32(5):507-522. doi: 10.1080/13543776.2022.2045947. Epub 2022 Mar 11. PMID: 35202550.
4: Grieselhuber NR, Mims AS. Novel Targeted Therapeutics in Acute Myeloid Leukemia: an Embarrassment of Riches. Curr Hematol Malig Rep. 2021 Apr;16(2):192-206. doi: 10.1007/s11899-021-00621-9. Epub 2021 Mar 18. PMID: 33738705; PMCID: PMC8515252.
5: AML Prognoses Better with Menin-MLL Inhibitor? Cancer Discov. 2021 Feb;11(2):216-217. doi: 10.1158/2159-8290.CD-NB2020-120. Epub 2020 Dec 30. PMID: 33380450.
