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
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
Preparing Stock Solutions
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 |
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.
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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.