Entospletinib (GS-9973)

Catalog No.S7523

Entospletinib (GS-9973) Chemical Structure

Molecular Weight(MW): 411.46

Entospletinib (GS-9973) is an orally bioavailable, selective Syk inhibitor with IC50 of 7.7 nM in a cell-free assay and showed 13- to >1000-fold cellular selectivity for Syk over other kinases(including Jak2, ckit, Flt3, Ret, KDR) as assessed by target protein phosphorylation or functional response.

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2 Customer Reviews

  • TF-1 cells were stimulated with EPO (10 U/ml) or GM-CSF (10 ng/ml), either in the absence or presence of R406 (1 μM) or GS-9973 (1 μM) for indicated time periods. Total cell lysates were analyzed by immunoblotting using indicated antibodies.

    Biochim Biophys Acta, 2017, 1864(4):687-696. Entospletinib (GS-9973) purchased from Selleck.

    (A) FcγRIIB+ Ramos cells were pre-treated with Syk inhibitor Entospletinib (GS-9973) then stimulated for 5 min with the indicated anti-IgM antibody, lysed and subjected to co-immuoprecipitation with specific antibody or isotype control. Eluates were separated by SDS-PAGE and western blotting was performed with the indicated antibodies.

    J Immunol, 2016, 197(5):1587-96.. Entospletinib (GS-9973) purchased from Selleck.

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Biological Activity

Description Entospletinib (GS-9973) is an orally bioavailable, selective Syk inhibitor with IC50 of 7.7 nM in a cell-free assay and showed 13- to >1000-fold cellular selectivity for Syk over other kinases(including Jak2, ckit, Flt3, Ret, KDR) as assessed by target protein phosphorylation or functional response.
Features Orally bioavailable Syk-selective inhibitor that has been tested in Phase II clinical trials for treatment of Haematological Malignancies.
Targets
Syk [1]
(Cell-free assay)
7.7 nM
In vitro

GS-9973 shows good bidirectional permeability across Caco-2 cell monolayers in vitro. In cells, GS-9973 also shows excellent selectivity for Syk, and potently inhibits BCR-mediated activation and proliferation of B-cells as well as immune-complex-stimulated cytokine production in monocytes. [1] The combination of idelalisib and GS-9973 synergistically inhibits CLL cell viability and further disrupts chemokine signaling. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human MV411 cells  MVrQdo9tcW[ncnH0bY9vKGG|c3H5 MYi3NkBp M2HnU2lvcGmkaYTpc44hd2ZiRnz0N{BqdiCqdX3hckBOXjRzMTDj[YxteyCjc4Pld5Nm\CCjczDhd5Nme3OnZDDhd{Bxem:uaX\ldoF1cW:wIHHmeIVzKDd{IHjyd{BqdmO3YnH0bY9vKGK7IIPw[YN1em:yaH;0c41mfHK7LDDFR|UxRTBwM{K3JO69VQ>? MViyOFc4QTVzNB?=
C57BL/6 mouse bone marrow cells NGHzPZREgXSxdH;4bYPDqGG|c3H5 MYW0JIRigXN? MXfDfZRwfG:6aXPpeJkh[WejaX7zeEBEPTeETD:2JI1wfXOnIHLvcoUhdWG{cn;3JINmdGy|IHHzd4V{e2WmIHHzJIdzd3e2aDDpcohq[mm2aX;uJJBz\WmwY4XiZZRm\CCob4KgOEBl[Xm|IH\vcIxwf2WmIHL5JHs{UF1vdHj5cYllcW6nIHHk[Il1cW:wIH3lZZN2emWmIHHmeIVzKDViaILzJIJ6KGKndHHwcIF1\SClb4XueIlv\yCjbnHsfZNqeyxiSVO1NF0xNjV6MjFOwG0> MWOyOVY{Ozd2MR?=

... Click to View More Cell Line Experimental Data

In vivo GS-9973 (1 mg/kg p.o.) shows moderate to high bioavailability in rat and dog. In a rat collagen-induced arthritis model, GS-9973 (1-10 mg/kg p.o.) significantly inhibits ankle inflammation. Moreover, GS-9973 also shows disease-modifying activity in multiple histological measurements, including inhibition of pannus formation, cartilage damage, bone resorption, and peritosteal bone formation with ED50 ranging from 1.2 to 3.9 mg/kg . [1]

Protocol

Kinase Assay:

[1]

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Kinase Assays:

Full-length baculovirus-expressed Syk kinase activity is measured in a Lance-based assay format in a final volume of 25 μL containing 25 mM Tris–HCl, pH 7.5, 5 mM β-glycerophosphate, 2 mM DTT, 0.1 mM Na3VO4, 10 mM MgCl2, 0.5 μM Promega PTK biotinylated peptide substrate 1, 0.01% casein, 0.01% Triton X-100, 0.25% glycerol, and 40 mM ATP (Km for ATP) incubated at room temperature for 60 min. Reactions are stopped with the addition of 30 mM EDTA containing 30 μL of SA-APC and 4 nM PT-66 antibody and the plates measured on a Perkin-Elmer Envision. IC50 values for test compounds are determined using a four-parameter linear regression algorithm.
Cell Research:

[1]

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  • Cell lines: MV-4-11 cells
  • Concentrations: ~10 μM
  • Incubation Time: 72 hours
  • Method:

    Functional impact on cellular Flt3 activity is determined by measuring compound inhibition of MV-4-11 cell proliferation. A total of 104 cells are diluted in RPMI medium containing 10% FBS in 96-well flat-bottomed tissue culture plates and incubated with compound dilutions for 72 h at 37 癈. Alamar blue (10%) is added to the cells, which were incubated for an additional 12-18 h at 37 癈, and inhibition of the relative cell numbers is determined by spectrophotometer readings at 570/600 nm.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: Rat Collagen-Induced Arthritis (CIA) Model
  • Formulation: Cremophor/ethanol/saline
  • Dosages: ~10 mg/kg bid
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 26 mg/mL warmed (63.18 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
4% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
2.5mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 411.46
Formula

C23H21N7O

CAS No. 1229208-44-9
Storage powder
in solvent
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

  • Question 1:

    How should we use S7523 to perform intraperitoneal injection in mice?

  • Answer:

    S7523 can be dissolved in 4% DMSO/30% PEG 300/5% Tween 80/ddH2O at up to 2.5mg/ml and use it for intra peritoneal injection in mice. When making this vehicle, please dissolve the product in DMSO first, then add PEG 300 and Tween 80 and dilute with water as a final step.

Syk Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID