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GSK2141795 hydrochloride

CAS# 1047635-80-2

GSK2141795 hydrochloride

Catalog No. BCC5295----Order now to get a substantial discount!

Product Name & Size Price Stock
GSK2141795 hydrochloride:1mg $156.00 In stock
GSK2141795 hydrochloride:2mg $265.00 In stock
GSK2141795 hydrochloride:5mg $624.00 In stock
GSK2141795 hydrochloride:10mg $1092.00 In stock
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Quality Control of GSK2141795 hydrochloride

Quality Control & MSDS

Number of papers citing our products

Chemical structure

GSK2141795 hydrochloride

3D structure

Chemical Properties of GSK2141795 hydrochloride

Cas No. 1047635-80-2 SDF Download SDF
PubChem ID 73330428 Appearance Powder
Formula C18H17Cl3F2N4O2 M.Wt 465.71
Type of Compound N/A Storage Desiccate at -20°C
Synonyms Uprosertib hydrochloride
Solubility Soluble in DMSO
Chemical Name N-[(2S)-1-amino-3-(3,4-difluorophenyl)propan-2-yl]-5-chloro-4-(4-chloro-2-methylpyrazol-3-yl)furan-2-carboxamide;hydrochloride
SMILES CN1C(=C(C=N1)Cl)C2=C(OC(=C2)C(=O)NC(CC3=CC(=C(C=C3)F)F)CN)Cl.Cl
Standard InChIKey LAPFKCIDRPWAFU-PPHPATTJSA-N
Standard InChI InChI=1S/C18H16Cl2F2N4O2.ClH/c1-26-16(12(19)8-24-26)11-6-15(28-17(11)20)18(27)25-10(7-23)4-9-2-3-13(21)14(22)5-9;/h2-3,5-6,8,10H,4,7,23H2,1H3,(H,25,27);1H/t10-;/m0./s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Protocol

Kinase Assay [1]
For 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.

References:
[1]. Pachl F, et al. Characterization of a chemical affinity probe targeting Akt kinases. J Proteome Res. 2013 Aug 2;12(8):3792-800.

GSK2141795 hydrochloride Dilution Calculator

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GSK2141795 hydrochloride Molarity Calculator

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Preparing Stock Solutions of GSK2141795 hydrochloride

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.1473 mL 10.7363 mL 21.4726 mL 42.9452 mL 53.6815 mL
5 mM 0.4295 mL 2.1473 mL 4.2945 mL 8.589 mL 10.7363 mL
10 mM 0.2147 mL 1.0736 mL 2.1473 mL 4.2945 mL 5.3681 mL
50 mM 0.0429 mL 0.2147 mL 0.4295 mL 0.8589 mL 1.0736 mL
100 mM 0.0215 mL 0.1074 mL 0.2147 mL 0.4295 mL 0.5368 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on GSK2141795 hydrochloride

GSK2141795 hydrochloride is a potent and selective pan-Akt inhibitor with IC50 values of 180/328/38 nM for Akt1/Akt2/Akt3, respectively.

In Vitro:GSK2141795 inhibits Akt1/2/3 with the Kd values of 16/49/5 nM, respectively. GSK2141795 potently inhibits only the PKC family members PRKACA and PRKACB as well as the cGMP-dependent protein kinase PRKG1 aqpart from the Akts. Protein targets that bind GSK2141795 in the lysate show a dose-dependent reduction in binding to the kinobeads, while proteins unaffected by the drug show no reduction in binding[1].

References:
[1]. Pachl F, et al. Characterization of a chemical affinity probe targeting Akt kinases. J Proteome Res. 2013 Aug 2;12(8):3792-800.

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Description

GSK2141795 Hcl is a potent and selective pan-Akt inhibitor with IC50 values of 180 nM for Akt1, 328 nM for Akt2, and 38 nM for Akt3 respectively (Clinical phase 1).

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