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Cat. No.: HY-15968A

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Entospletinib dimesylate

Name: Entospletinib dimesylate
Brand: MedChemExpress
SKU: HY-15968A
Availability: PreOrder

(Synonyms: GS-9973 dimesylate)

12 Cited Publications

Customer Review

Based on 12 publication(s) in Google Scholar

Entospletinib dimesylate (GS-9973 dimesylate) is an orally bioavailable, selective Syk inhibitor with an IC₅₀ of 7.7 nM.

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

CAS No.: 1648797-46-9
Formula: C₂₅H₂₉N₇O₇S₂
Molecular Weight:603.67

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Entospletinib dimesylate Chemical Structure

CAS No.: 1648797-46-9

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (12)
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

Entospletinib dimesylate (GS-9973 dimesylate) is an orally bioavailable, selective Syk inhibitor with an IC₅₀ of 7.7 nM.

IC₅₀ & Target

IC50: 7.7 nM (Syk)

In Vitro

Entospletinib dimesylate (GS-9973 dimesylate) shows good bidirectional permeability across Caco-2 cell monolayers in vitro. In cells, Entospletinib dimesylate 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 (HY-13026) and Entospletinib dimesylate synergistically inhibits CLL cell viability and further disrupts chemokine signaling^[2].

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

In Vivo

Entospletinib (1 mg/kg, p.o.) dimesylate (GS-9973 dimesylate) shows moderate to high bioavailability in rat and dog. In a rat collagen-induced arthritis model, Entospletinib (1-10 mg/kg, p.o.) dimesylate significantly inhibits ankle inflammation. Moreover, Entospletinib dimesylate 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].

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

Chemical Information

CAS No. 1648797-46-9
Molecular Weight 603.67
Formula C₂₅H₂₉N₇O₇S₂
SMILES

O=S(O)(C)=O.O=S(O)(C)=O.C1(C=NN2)=C2C=C(C3=CN4C=CN=C4C(NC5=CC=C(N6CCOCC6)C=C5)=N3)C=C1
Synonyms

GS-9973 dimesylate
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Publications (12)

All In Vivo Efficacy StudyIn Vivo ImagingIHC

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Journal Impact Factor

Nat Commun

Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]

2026 Feb 12;17(1):1214. PMID: 41680175
Cell Rep

Integrated metabolic-transcriptomic network identifies immunometabolic modulations in human macrophages. [Abstract]

2024 Sep 13;43(9):114741. PMID: 39276347
Cell Rep

Podocyte SIRPα reduction aggravates lupus nephritis via promoting T cell inflammatory responses. [Abstract]

2024 May 16;43(5):114249. PMID: 38758648
Mol Cancer Ther

AKT Inhibition Sensitizes to Polo-Like Kinase 1 Inhibitor Onvansertib in Prostate Cancer. [Abstract]

2024 Oct 1;23(10):1404-1417. PMID: 38894678
Eur J Med Chem

Scaffold hopping of the SYK inhibitor entospletinib leads to broader targeting of the BCR signalosome. [Abstract]

2020 Oct 15:204:112636. PMID: 32731189
J Bone Miner Res

Alveolar Bone Protection by Targeting the SH3BP2-SYK Axis in Osteoclasts. [Abstract]

2020 Feb;35(2):382-395. PMID: 31613396
J Bone Miner Res

Second-Generation SYK Inhibitor Entospletinib Ameliorates Fully Established Inflammation and Bone Destruction in the Cherubism Mouse Model. [Abstract]

2018 Aug;33(8):1513-1519. PMID: 29669173

Entospletinib dimesylate purchased from MedChemExpress. Usage Cited in: J Bone Miner Res. 2018 Aug;33(8):1513-1519. [Abstract]

Experimental sequence of Entospletinib (GS-9973, 100 mg/kg, daily) administration. 10-week-old Sh3bp2^+/+ and Sh3bp2^KI/KI mice were treated with 100 mg/kg of GS-9973 or DMSO every day for 6 weeks. Mice were euthanized at 16 weeks of age for analysis.

Entospletinib dimesylate purchased from MedChemExpress. Usage Cited in: J Bone Miner Res. 2018 Aug;33(8):1513-1519. [Abstract]

Facial appearance of Entospletinib (GS-9973, 100 mg/kg, daily)- treated or DMSO-treated mice (top: before treatment at 10 weeks of age; bottom: after treatment at 16 weeks of age). Blue arrows indicate closed eyelids due to facial skin inflammation. GS-9973 treatment improved eyelid closure in Sh3bp2^KI/KI mice at 16 weeks old (red arrows). Numbers represent the percentage of Sh3bp2^KI/KI mice with improved facial swelling.

Entospletinib dimesylate purchased from MedChemExpress. Usage Cited in: J Bone Miner Res. 2018 Aug;33(8):1513-1519. [Abstract]

Liver sections from Entospletinib (GS-9973, 100 mg/kg, daily)-treated or DMSO-treated Sh3bp2^+/+ and Sh3bp2^KI/KI mice (H&E). Arrows indicate inflammatory infiltrates.

Entospletinib dimesylate purchased from MedChemExpress. Usage Cited in: J Bone Miner Res. 2018 Aug;33(8):1513-1519. [Abstract]

Serum TNF-α levels of GS-9973-treated or DMSO-treated Sh3bp2^+/+ and Sh3bp2^KI/KI mice at 16 weeks old.

Entospletinib dimesylate purchased from MedChemExpress. Usage Cited in: J Bone Miner Res. 2018 Aug;33(8):1513-1519. [Abstract]

3D μCT images of the ankle joint (top) and calcaneus (bottom) from 16-week-old Sh3bp2^+/+ and Sh3bp2^KI/KI mice treated with Entospletinib (GS-9973) or DMSO.
J Mol Cell Biol

FcεRIγ Reinforces Double-Negative T cell-mediated Antibody-dependent Cellular Cytotoxicity Against Tumor Cells. [Abstract]

2026 Jan 2:mjaf059. PMID: 41481135
Hematol Oncol

Gene Expression Profiling in Acute Myeloid Leukemia Patient Subgroups With High and Low Sensitivity Toward SYK Inhibitors. [Abstract]

2025 Mar;43(2):e70058. PMID: 40088478
Metabolomics

2026 Apr 17;22(3):51.
PLoS One

A novel small molecule screening assay using normal human chondrocytes toward osteoarthritis drug discovery. [Abstract]

2024 Nov 1;19(11):e0308647. PMID: 39485774
SSRN

2023 Dec 1.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Currie KS, et al. Discovery of GS-9973, a Selective and Orally Efficacious Inhibitor of Spleen Tyrosine Kinase. J Med Chem. 2014 May 8;57(9):3856-73. [Content Brief]

[2]. Burke RT, et al. A potential therapeutic strategy for chronic lymphocytic leukemia by combining Idelalisib and GS-9973, a novel spleen tyrosine kinase (Syk) inhibitor. Oncotarget. 2014 Feb 28;5(4):908-15. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Keywords

Entospletinib dimesylate

12 Cited Publications

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (12)
Purity & Documentation
References

1/16
1/16

Entospletinib dimesylate purchased from MedChemExpress. Usage Cited in: J Bone Miner Res. 2018 Aug;33(8):1513-1519. [Abstract]

Customer Validation
Experimental sequence of Entospletinib (GS-9973, 100 mg/kg, daily) administration. 10-week-old Sh3bp2^+/+ and Sh3bp2^KI/KI mice were treated with 100 mg/kg of GS-9973 or DMSO every day for 6 weeks. Mice were euthanized at 16 weeks of age for analysis.
1/16

Entospletinib dimesylate purchased from MedChemExpress. Usage Cited in: J Bone Miner Res. 2018 Aug;33(8):1513-1519. [Abstract]

Customer Validation
Facial appearance of Entospletinib (GS-9973, 100 mg/kg, daily)- treated or DMSO-treated mice (top: before treatment at 10 weeks of age; bottom: after treatment at 16 weeks of age). Blue arrows indicate closed eyelids due to facial skin inflammation. GS-9973 treatment improved eyelid closure in Sh3bp2^KI/KI mice at 16 weeks old (red arrows). Numbers represent the percentage of Sh3bp2^KI/KI mice with improved facial swelling.
1/16

Entospletinib dimesylate purchased from MedChemExpress. Usage Cited in: J Bone Miner Res. 2018 Aug;33(8):1513-1519. [Abstract]

Customer Validation
Liver sections from Entospletinib (GS-9973, 100 mg/kg, daily)-treated or DMSO-treated Sh3bp2^+/+ and Sh3bp2^KI/KI mice (H&E). Arrows indicate inflammatory infiltrates.
1/16

Entospletinib dimesylate purchased from MedChemExpress. Usage Cited in: J Bone Miner Res. 2018 Aug;33(8):1513-1519. [Abstract]

Customer Validation
Serum TNF-α levels of GS-9973-treated or DMSO-treated Sh3bp2^+/+ and Sh3bp2^KI/KI mice at 16 weeks old.
1/16

Entospletinib dimesylate purchased from MedChemExpress. Usage Cited in: J Bone Miner Res. 2018 Aug;33(8):1513-1519. [Abstract]

Customer Validation
3D μCT images of the ankle joint (top) and calcaneus (bottom) from 16-week-old Sh3bp2^+/+ and Sh3bp2^KI/KI mice treated with Entospletinib (GS-9973) or DMSO.

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Entospletinib dimesylate

Publications Citing Use of MedChemExpress (MCE) Entospletinib dimesylate

Biological Activity

Chemical Information

Publications (12)

Purity & Documentation

References

Calculators

Help & FAQs

Entospletinib dimesylate Related Classifications

HY-15968A Related Classifications

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