[CAS NO. 1401966-69-5] GSK2879552

Name: GSK2879552
Brand: Arctom Scientific
SKU: AS936423

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PRODUCTS SPECIFICATIONS [1401966-69-5]

Distributor

Catalog

AS936423

Brand

Arctom Scientific

CAS

1401966-69-5

DESCRIPTION [1401966-69-5]

Overview

MDL	MFCD28411435
Molecular Weight	364.48
Molecular Formula	C23H28N2O2
SMILES	O=C(O)C1=CC=C(CN2CCC(CN[C@H]3[C@H](C4=CC=CC=C4)C3)CC2)C=C1

For research use only. We do not sell to patients.

7 Publications Citing Use of MCE

Summary

GSK2879552 an orally active, selective and irreversible inhibitor of lysine specific demethylase 1 (LSD1/ KDM1A) , with potential antineoplastic activity ^[1] ^[2] .

In Vitro

GSK2879552 inhibits KDM1A histone demethylase activity, inducing differentiation of sorafenib-resistant cells and attenuates stemness properties. GSK2879552 depresses the transcription of Wnt antagonists and downregulates β-catenin signaling activity in sorafenib-resistant cells ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay ^[2] .

Cell Line:	9/28 small cell lung carcinoma (SCLC) lines and 20/29 AML lines.
Concentration:	0-10000 nM.
Incubation Time:	6 days.
Result:	Inhibited cell proliferation.

RT-PCR ^[1] .

Cell Line:	Resistant HCC cells (PLC/PRF/5 and Huh7).
Concentration:	0, 1, 2 μM.
Incubation Time:	24 h.
Result:	Displayed reduced mRNA expression levels of stem cell markers, such as Lgr5, Sox9, Nanog and CD90, and elevated mRNA expression levels of differentiation markers Alb and Hnf4.

In Vivo

GSK2879552 (1.5 mg/kg, p.o.) treatment exhibits tumor growth inhibition in SCLC xenograft bearing mice ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	NCI-H526 and NCI-H1417 xenografts ^[2] .
Dosage:	1.5 mg/kg.
Administration:	PO daily for 25-35 days.
Result:	There was 57% and 83% tumor growth inhibition (TGI) in NCI-H526 and NCI-H1417 tumor bearing mice respectively. NCI-H510 and NCI-H69 tumor bearing mice also demonstrated partial TGI (38% and 49% respectively) in response to GSK2879552, while no significant TGI was observed for SHP77 bearing mice.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT02929498	GlaxoSmithKline\|Parexel	Myelodysplastic Syndrome\|Myelodysplastic Syndromes	July 31, 2017	Phase 1\|Phase 2
NCT02177812	GlaxoSmithKline	Leukaemia, Myelocytic, Acute	August 27, 2014	Phase 1
NCT02034123	GlaxoSmithKline	Carcinoma, Small Cell	February 4, 2014	Phase 1

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL ( 137.18 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.7436 mL	13.7182 mL	27.4363 mL
5 mM	0.5487 mL	2.7436 mL	5.4873 mL
10 mM	0.2744 mL	1.3718 mL	2.7436 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.75 mg/mL (7.54 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.75 mg/mL (7.54 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.75 mg/mL (7.54 mM); Clear solution

* All of the co-solvents are available by MCE.