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Seclidemstat

Cat. No. M9689
Seclidemstat Structure
Synonym:

SP-2577

Size Price Availability Quantity
10mg USD 150  USD150 In stock
25mg USD 320  USD320 In stock
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Quality Control & Documentation
Biological Activity

Seclidemstat is an orally active, reversible, noncompetitive inhibitor of lysine-specific demethylase 1 (LSD1, or KDM1A) with a mean IC50 of 127 nM, it has potential antineoplastic activity. Seclidemstat suppresses the expression of target genes by converting the di- and mono-methylated forms of lysine at position 4 of histone 3 (H3K4) to mono- and unmethylated H3K4, respectively.

In vivo, Seclidemstat reduces tumor volume at 40, 80 mg/kg by i.p. and also shows such effect at 80 mg/kg via p.o. dosing.

Chemical Information
Molecular Weight 450.94
Formula C20H23ClN4O4S
CAS Number 1423715-37-0
Solubility (25°C) DMSO ≥ 90 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Raushan T Kurmasheva, et al. Pediatr Blood Cancer. In vivo evaluation of the lysine-specific demethylase (KDM1A/LSD1) inhibitor SP-2577 (Seclidemstat) against pediatric sarcoma preclinical models: A report from the Pediatric Preclinical Testing Consortium (PPTC)

[2] Xing-Jie Dai, et al. J Med Chem. Reversible Lysine Specific Demethylase 1 (LSD1) Inhibitors: A Promising Wrench to Impair LSD1

[3] Cavan P Bailey, et al. Front Immunol. Scaffolding LSD1 Inhibitors Impair NK Cell Metabolism and Cytotoxic Function Through Depletion of Glutathione

[4] Raffaella Soldi, et al. PLoS One. The novel reversible LSD1 inhibitor SP-2577 promotes anti-tumor immunity in SWItch/Sucrose-NonFermentable (SWI/SNF) complex mutated ovarian cancer

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Keywords: Seclidemstat, SP-2577 supplier, Histone demethylase, inhibitors, activators


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