GSK2636771 - Moligand™, 10mM in DMSO , PI3-kinase p110-beta subunit inhibitor, CAS No.1372540-25-4, PI3-kinase p110-beta subunit inhibitor

CAS: 1372540-25-4 Cat. No.: G409258 Molecular Weight: 433.42

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

1H-Benzimidazole-4-carboxylic acid, 2-methyl-1-[[2-methyl-3-(trifluoromethyl)phenyl]methyl]-6-(4-morpholinyl)-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

GSK2636771 is a potent, orally bioavailable and selective inhibitor ofPI3Kβwith >900-fold selectivity over PI3Kα/PI3Kγ and >10-fold over PI3Kδ. Sensitive to PTEN cell lines.
In vitro

GSK-2636771 shows selectively inhibitory activity in PTEN cell lines (human prostate adenocarcinoma PC-3 and breast cancer HCC70) with EC50 of 36 nM and 72 nM, respectively. GSK2636771 significantly decreases cell viability in p110β-reliant PTEN-deficient PC3 prostate and BT549 and HCC70 breast cancer cell lines, and leads to a marked decrease of AKT phosphorylation only in the control prostate and breast cancer cell lines.

In vivo

GSK-2636771 decreases phosphorylated protein kinase Akt (Ser473) levels in these xenograft models. GSK-2636771 (100 mg/kg) do not increase glucose/insulin levels in mice.
Cell Data

cell lines：MALME-3M, Colo829, Colo38, A375, SK-MEL28, and A2058 cells

Concentrations：~10 μM

Incubation Time：72 hours

Powder Purity:≥99%

Specifications

Synonyms

1H-Benzimidazole-4-carboxylic acid, 2-methyl-1-[[2-methyl-3-(trifluoromethyl)phenyl]methyl]-6-(4-morpholinyl)-

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

GSK2636771 is a potent, orally bioavailable and selective inhibitor of PI3Kβ with >900-fold selectivity over PI3Kα/PI3Kγ and >10-fold over PI3Kδ. Sensitive to PTEN null cell lines.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

INHIBITOR

Mechanism of action

PI3-kinase p110-beta subunit inhibitor

Product Properties

• ALogP: 4

Names and Identifiers

• Isomeric SMILES: CC1=C(C=CC=C1C(F)(F)F)CN2C(=NC3=C(C=C(C=C32)N4CCOCC4)C(=O)O)C
• Molecular Weight: 433.42
• Reaxy-Rn: 22377911
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=22377911&ln=

Associated Targets(Human)

PIK3CB Tchem Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform (4 Activities)

Discover Target: PIK3CB

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Chemical and Physical Properties

• Solubility: Solubility (25°C) In vitro DMF 24 mg/mL warmed with 50ºC Water: bath (51.65 mM); DMSO: 0.01 mg/mL warmed with 50ºC Water: bath (0.02 mM); Water: Insoluble