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Seclidemstat (SP-2577) LSD1 inhibitor

Cat.No.S6722

Seclidemstat (SP-2577) is a potent and orally bioavailable inhibitor of lysine-specific demethylase 1 (LSD1/KDM1A) with IC50 of 13 nM. This compound has potential antineoplastic activity.
Seclidemstat (SP-2577) LSD1 inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 450.94

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Quality Control

Batch: Purity: 99.72%
99.72

Solubility

In vitro
Batch:

DMSO : 90 mg/mL (199.58 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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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 ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 450.94 Formula

C20H23ClN4O4S

Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1423715-37-0 -- Storage of Stock Solutions

Synonyms SP-2577 mesylate Smiles CC(=NNC(=O)C1=CC(=CC=C1)S(=O)(=O)N2CCN(CC2)C)C3=C(C=CC(=C3)Cl)O

Mechanism of Action

Targets/IC50/Ki
LSD1/KDM1A
(Cell-free assay)
13 nM
In vitro

The combination therapy of Seclidemstat (SP-2577) with checkpoint inhibitors may induce or augment immunogenic responses of SWI/SNF-mutated ovarian cancers. This compound promotes endogenous retroviruses (ERVs) expression and activation of IFNβ pathway in small cell carcinoma of the ovary hypercalcemic type (SCCOHT) cell lines. It (3 μM) promotes PD-L1 expression in SCCOHT COV 434 pIND 20 BRG1-2.7 cell line.

In vivo

SP-2577 (Seclidemstat) is an inhibitor of lysine-specific demthylase KDM1A (LSD1) potential antineoplastic activity against pediatric sarcomas.

References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04611139 Withdrawn
SCCOHT|Ovarian Clear Cell Tumor|Ovarian Endometrioid Adenocarcinoma|Endometrial Cancer
HonorHealth Research Institute|Merck Sharp & Dohme LLC|Salarius Pharmaceuticals LLC
December 31 2021 Phase 1
NCT03895684 Completed
Advanced Solid Tumors
Salarius Pharmaceuticals LLC
June 25 2019 Phase 1
NCT03600649 Active not recruiting
Ewing Sarcoma|Myxoid Liposarcoma|SarcomaSoft Tissue|Desmoplastic Small Round Cell Tumor|Extraskeletal Myxoid Chondrosarcoma|Angiomatoid Fibrous Histiocytoma|Clear Cell Sarcoma|Primary Pulmonary Myxoid Sarcoma|Myoepithelial Tumor|Sclerosing Epithelioid Fibrosarcoma|Fibromyxoid Tumor
Salarius Pharmaceuticals LLC|National Pediatric Cancer Foundation
June 4 2018 Phase 1

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