[CAS NO. 1902123-72-1] GSK2879552 2HCl
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PRODUCTS SPECIFICATIONS [1902123-72-1]
Catalog
SLK-S7796
Brand
Selleck
CAS
1902123-72-1
DESCRIPTION [1902123-72-1]
Overview
| MDL | MFCD30481342 |
|---|---|
| Molecular Weight | 437.4 |
| Molecular Formula | C23H28N2O2.2HCl |
| SMILES | O=C(O)C1=CC=C(CN2CCC(CN[C@H]3[C@H](C4=CC=CC=C4)C3)CC2)C=C1.[H]Cl.[H]Cl |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2862 mL | 11.4312 mL | 22.8624 mL |
| 5 mM | 0.4572 mL | 2.2862 mL | 4.5725 mL |
| 10 mM | 0.2286 mL | 1.1431 mL | 2.2862 mL |
| 50 mM | 0.0457 mL | 0.2286 mL | 0.4572 mL |
Description
GSK2879552 2HCl is a potent, selective, orally bioavailable, irreversible inhibitor with of 1.7 μM. Phase 1.
Targets
| LSD1 [1] (Cell-free assay) |
| 1.7 μM(Ki) |
In vitro
In 165 cell lines, GSK2879552 inhibits the growth of 9/28 small cell lung carcinoma (SCLC) lines and 20/29 AML lines ranged from 40% to 100%. The subset of SCLC lines and primary samples that undergo growth inhibition in response to GSK2879552 exhibit DNA hypomethylation of a signature set of probes.
In vivo
In SCLC xenograft bearing mice, GSK2879552 (1.5 mg/kg, p.o.) demonstrates tumor growth inhibition by 17%-83%.
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