2604513-16-6
Chemical Structure
Gintemetostat
Synonym(s): KTX-1001
- CAS No.: 2604513-16-6
- Formula:C25H26F4N8O2
- Molecular Weight:546.52
IUPAC Name: (S)-1-((R)-3-amino-1-(4-((6-amino-9H-purin-9-yl)methyl)-6-(2,5-difluoro-4-methoxyphenyl)pyridin-3-yl)piperidin-3-yl)-2,2-difluoroethan-1-ol
InChIKey: PIFXSVGCYBHXHR-PXDATVDWSA-N
SMILES: FC(C=C(C(F)=C1)OC)=C1C2=NC=C(N3C[C@](N)(CCC3)[C@H](O)C(F)F)C(CN4C5=NC=NC(N)=C5N=C4)=C2
Biological Activity: Gintemetostat (KTX-1001) is an orally active, highly specific NSD2/MMSET histone methyltransferase inhibitor with human NSD2 IC50 values ranging 0.460-2.17 nM and NSD2 SET domain IC50 of 2.32 nM and Kd values ranging 6.3-70.4 nM[1][4].Gintemetostat reduces H3K36me2 levels, impairs multiple myeloma cell adhesion and colony formation, enhances cytotoxicity, boosts T-cell activation, and sensitizes resistant multiple myeloma cells to other agents[1][2][6].Gintemetostat can be used for the research of multiple myeloma and relapsed and refractory multiple myeloma[1][2][3][4][5][6].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Gintemetostat | 99.81% | Gintemetostat (KTX-1001) is an orally active, highly specific NSD2/MMSET histone methyltransferase inhibitor with human NSD2 IC50 values ranging 0.460-2.17 nM and NSD2 SET domain IC50 of 2.32 nM and Kd values ranging 6.3-70.4 nM.Gintemetostat reduces H3K36me2 levels, impairs multiple myeloma cell adhesion and colony formation, enhances cytotoxicity, boosts T-cell activation, and sensitizes resistant multiple myeloma cells to other agents.Gintemetostat can be used for the research of multiple myeloma and relapsed and refractory multiple myeloma. | ||||||||||||||||||||
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References
- [1]. Sridharan V, et al. Ktx-1001, a potent, selective MMSET/NSD2 inhibitor, enhances immunomodulatory and immune-directed therapies in preclinical models of multiple myeloma[J]. Blood, 2025, 146: 7456.
- [2]. Nandana D, et al. Anti-Adhesion Properties of KTX-1001, a Selective NSD2/MMSET Inhibitor, Enhance Carfilzomib Sensitivity in Multiple Myeloma[J]. Clinical Lymphoma, Myeloma and Leukemia, 2025, 25: S213-S214.
- [3]. Berdeja J G, et al. Trial in Progress: A Phase 1 Study of KTX-1001, an Oral, First-in-Class, Selective MMSET Inhibitor in Patients with Relapsed and Refractory Multiple Myeloma[J]. Blood, 2023, 142: 3391.
- [4]. Lewis CA, et al. Characterization of the activity of KTX-1001, a small molecule inhibitor of multiple myeloma SET domain using surface plasmon resonance. J Biol Chem. 2025;301(7):110382. [Content Brief]
- [5]. Ma Z, et al. Drug Discovery Targeting Nuclear Receptor Binding SET Domain Protein 2 (NSD2). J Med Chem. 2023;66(16):10991-11026. [Content Brief]
- [6]. Flynt E, et al. Ktx-1029, a Potent, Selective MMSET/NSD2 Inhibitor Is Effective in t (4; 14) Multiple Myeloma Preclinical Models[J]. Blood, 2024, 144: 1878.
