KO-539 free base · Synonyms: Ziftomenib

Ziftomenib is a potent and selective menin inhibitor.

For research use only. Not for human or veterinary use.

Target Epigenetic Reader Domain

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

KO-539 structure

CAS No.: 2134675-36-6

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
100 mg	USD 480.00	BP-01973-100mg	In stock	Get quote
250 mg	USD 720.00	BP-01973-250mg	In stock	Get quote
500 mg	USD 980.00	BP-01973-500mg	In stock	Get quote
1 g	USD 1,280.00	BP-01973-1g	In stock	Get quote
5 g	Inquire	BP-01973-5g	Inquire	Inquire

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Description

Ziftomenib (KO-539) is a potent and selective menin inhibitor.

Biological activity

Ziftomenib (KO-539) is an orally active menin-MLL interaction inhibitor with antitumor activities (WO2017161028A1, compound 151). In Vitro 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.

Identifiers

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
InChIKey: BGGALFIXXQOTPY-NRFANRHFSA-N

Specifications

MW (average): 717.8710
Formula: C₃₃H₄₂F₃N₉O₂S₂
CAS No.: 2134675-36-6
Physical state: Solid
Color: Off-white to light yellow
Shipping: 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: Powder 4℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

References

[1]. Rausch, Johanna 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.” Haematologica vol. 108,10 2837-2843. 1 Oct. 2023, doi:10.3324/haematol.2022.282160

[2]. Tao Wu, et al. Substituted inhibitors of menin-mll and methods of use. WO2017161028A1.

Same target

Search Epigenetic Reader Domain

Same research area

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