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Uprosertib

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Purity:99.54%

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COA HPLC HNMR

Uprosertib

Catalog No. T6849Cas No. 1047634-65-0

Uprosertib (GSK2141795) (GSK2141795) is a selective, ATP-competitive, and orally bioavailable Akt inhibitor with IC50 of 180 nM, 328 nM, and 38 nM for Akt 1, 2 and 3, respectively. Phase 2.

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Pack Size	Price	Availability
1 mg	$39	In Stock
2 mg	$54	In Stock
5 mg	$77	In Stock
10 mg	$126	In Stock
25 mg	$212	In Stock
50 mg	$340	In Stock
100 mg	$563	In Stock
200 mg	$791	In Stock
1 mL x 10 mM (in DMSO)	$110	In Stock

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Product Introduction

Bioactivity

Description	Uprosertib (GSK2141795) (GSK2141795) is a selective, ATP-competitive, and orally bioavailable Akt inhibitor with IC50 of 180 nM, 328 nM, and 38 nM for Akt 1, 2 and 3, respectively. Phase 2.
In vitro	Uprosertib inhibits multiple AKT substrate phosphorylation levels, including GSK3β, PRAS40, FOXO and Caspase 9 in both BT474 and LNCaP cells. Uprosertib preferentially inhibits the proliferation of human cancer cells lines with AKT pathway activation. In LNCaP, BT474, A3 and I9.2 cells lines, Uprosertib also causes cell cycle arrest. [2] In both SKOV3 and PEO4 cells, Uprosertib causes growth-arrest as single agent, and enhances cisplatin-induced apoptosis. [3]
In vivo	In mice bearing BT474 breast tumor xenografts, Uprosertib (100 mg/kg, p.o.) results 61% tumor growth inhibition. In mice bearing SKOV3 ovarian tumor xenografts, Uprosertib (30 mg/kg, p.o.) results 61% tumor growth inhibition. [2]
Kinase Assay	Selectivity profiling experiments: The lysates (5 mg of total protein each) are preincubated with 0 (DMSO control), 2.5 nM, 25 nM, 250 nM, 2.5 μM or 25 μM free compound (GSK690693 or GSK2141795) on an end-over-end shaker for 45 min at 4 °C. Subsequently, lysates are incubated with beads (coupled Akt probe or kinobeads) for 1 h at 4 °C, for both qualitative and quantitative experiments. The beads are washed with 1× CP buffer and collected by centrifugation. Bound proteins are eluted with 2× NuPAGE LDS sample buffer, and eluates are reduced and alkylated by 50 mM dithiothreitol and 55 mM iodoacetamide.
Cell Research	Cell lines are typically grown in RPMI 160 medium containing 10% FBS. Some cell lines are grown in media specified by the vendor. A 3-day proliferation assay using CellTiter-Glo is performed to measure the growth inhibition by the compounds at 0–30 μM. Cell growth is determined relative to untreated (DMSO) controls. EC50's are calculated from inhibition curves using a 4- or 6-parameter fitting algorithm in the Assay Client application.(Only for Reference)
Alias	GSK2141795, GSK795

Chemical Properties

Molecular Weight	429.25
Formula	C18H16Cl2F2N4O2
Cas No.	1047634-65-0

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 76 mg/mL(177.1 mM)

DMSO: 65 mg/mL (151.43 mM)

Solution Preparation Table

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	2.3296 mL	11.6482 mL	23.2964 mL	116.4822 mL
5 mM	0.4659 mL	2.3296 mL	4.6593 mL	23.2964 mL
10 mM	0.2330 mL	1.1648 mL	2.3296 mL	11.6482 mL
20 mM	0.1165 mL	0.5824 mL	1.1648 mL	5.8241 mL
50 mM	0.0466 mL	0.2330 mL	0.4659 mL	2.3296 mL
100 mM	0.0233 mL	0.1165 mL	0.2330 mL	1.1648 mL

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