Name: Seclidemstat (SP-2577)
Brand: Selleck Chemicals
SKU: S6722
Rating: 5 (1 reviews)

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

Seclidemstat (SP-2577) Chemical Structure

CAS: 1423715-37-0

Selleck's Seclidemstat (SP-2577) has been cited by 1 publication

Purity & Quality Control

Batch: Purity: 99.72%

99.72

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Biological Activity

Description

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

Targets

LSD1/KDM1A ^[1]
(Cell-free assay)

13 nM

In vitro
In vitro	The combination therapy of Seclidemstat (SP-2577) with checkpoint inhibitors may induce or augment immunogenic responses of SWI/SNF-mutated ovarian cancers. Seclidemstat promotes endogenous retroviruses (ERVs) expression and activation of IFNβ pathway in small cell carcinoma of the ovary hypercalcemic type (SCCOHT) cell lines. Seclidemstat (3 μM) promotes PD-L1 expression in SCCOHT COV 434 pIND 20 BRG1-2.7 cell line.^[1]
Cell Research	Cell lines	Small cell carcinoma of the ovary hypercalcemic type (SCCOHT) cell lines, ovarian clear cell carcinomas (OCCC) cell lines
	Concentrations	1μM,3 μM
	Incubation Time	72 h
	Method	The SCCOHT and OCCC cell lines are seeded in T-25 tissue culture treated flasks at 3 x 10₅ cells in 5mL of the appropriate phenol red free complete growth medium. After 48 h, at 70–80% confluency, the cells are treated with 3μM or 1μM of Seclidemstat. After 72 h, the media is collected from the flasks and stored at -80°C until use for various assays.

In Vivo
In vivo	SP-2577 (Seclidemstat) is an inhibitor of lysine-specific demthylase KDM1A (LSD1) potential antineoplastic activity against pediatric sarcomas.
Animal Research	Animal Models	C.B.17SC scid−/− female mice
	Dosages	100 mg/kg
	Administration	i.p.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT04611139	Withdrawn	SCCOHT\|Ovarian Clear Cell Tumor\|Ovarian Endometrioid Adenocarcinoma\|Endometrial Cancer	HonorHealth Research Institute\|Merck Sharp & Dohme LLC\|Salarius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

References

Chemical Information & Solubility

Molecular Weight	450.94	Formula	C₂₀H₂₃ClN₄O₄S
CAS No.	1423715-37-0	SDF	--
Smiles	CC(=NNC(=O)C1=CC(=CC=C1)S(=O)(=O)N2CCN(CC2)C)C3=C(C=CC(=C3)Cl)O
Storage (From the date of receipt)	3 years -20°C powder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years -20°C powder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 90 mg/mL ( (199.58 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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% DMSO + % + % Tween 80 + % ddH₂O

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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