DATASHEET
Formulation
Powder
Storage:
Store in dry, dark place at -20C for 1 year.
Product Information:
Molecular Weight: 437.4
Formula: C23 H30 Cl2 N2 O2
CAS Number: 1902123-72-1
InChi Key: QEKGSBZKRLHQSZ-VSIGASKDSA-N
InChi: InChI=1S/C23H28N2O2.2ClH/c26-23(27)20-8-6-18(7-9-20)16-25-12-10-17(11-13-25)15-24-22-14-21(22)19-4-2-1-3-5-19;;/h1-9,17,21-22,24H,10-16H2,(H,26,27);2*1H/t21-,22+;;/m0../s1
Smiles: Cl.Cl.OC(=O)C1=CC=C(CN2CCC(CN[C@@H]3C[C@H]3C3C=CC=CC=3)CC2)C=C1
Purity: 98.0
Solubility: DMSO up to 50 mM; Water up to 50 mM
Appearance: Solid Power.
Shelf Life: 1.0 years
Description:
GSK2879552 is a highly potent, selective and orally bioavailable irreversible inhibitor of Lysine Specific Demethylase 1 (LSD1). It is highly selective over related enzymes such as MAO-A/B. A proliferation screen of cell lines representing a number of tumor types indicated that small cell lung carcinoma (SCLC) is sensitive to GSK2879552’s inhibition. It increases H3K4 methylation selectively at genomic regions bound by LSD1. It demonstrates efficacy in preclinical models of SCLC. Currently GSK2879552 is in phase I clinical trials targeting Acute Myeloid Leukemia (AML) and Relapsed/Refractory Small Cell Lung Carcinoma.