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Chemical Structure| 1229208-44-9 Chemical Structure| 1229208-44-9

Structure of Entospletinib
CAS No.: 1229208-44-9

Chemical Structure| 1229208-44-9

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GS-9973 is a Syk inhibitor with IC50 value of 7.7 nM which is used for the treatment of autoimmune and oncology indications.

Synonyms: GS-9973

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Product Citations

Nanae Asakawa ; Toshiaki Oharaseki ; Yuki Yokouchi ; Noriko Miura ; Naohito Ohno ; Kei Takahashi

Abstract: Background: The activation of innate immunity may be involved in the development of Candida albicans-induced murine vasculitis, which resembles Kawasaki disease (KD)vasculitis. This study aimed to histologically clarify the time course of the development of vasculitis in this model in detail and to estimate the potential role of (Syk) inhibitors in KD vasculitis. Methods and Results: DBA/2 male mice were intraperitoneally injected with a vasculitis_x005f_x0002_inducing substance and treated with a inhibitor (R788 or GS-9973). Systemic vasculitis, especially in the aortic annulus area, was histologically evaluated. Regarding lesions in the aortic annulus area, some mice in the untreated control group already showed initiation of vasculitis 1 day after the final injection of a vasculitis-inducing substance. The vasculitis expanded over time. Inflammation occurred more frequently at the aortic root than at the coronary artery. The distribution of inflammatory cells was limited to the intima, intima plus adventitia, or all layers. In the inhibitor-treated groups, only one mouse had vasculitis at all observation periods. The severity and area of the vasculitis were reduced by both inhibitors. Conclusion: Candida albicans-induced murine vasculitis may occur within 1 day after the injection of a vasculitis-inducing substance. Additionally, inhibitors suppress murine vasculitis.

Keywords: Kawasaki disease ; vasculitis ; Candida albicans ; murine model ;

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Product Details of Entospletinib

CAS No. :1229208-44-9
Formula : C23H21N7O
M.W : 411.46
SMILES Code : C12=NC=CN1C=C(C3=CC4=C(C=C3)C=NN4)N=C2NC5=CC=C(N6CCOCC6)C=C5
Synonyms :
GS-9973
MDL No. :MFCD28099806
InChI Key :XSMSNFMDVXXHGJ-UHFFFAOYSA-N
Pubchem ID :59473233

Safety of Entospletinib

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of Entospletinib

RTK

Isoform Comparison

Biological Activity

Target
  • Syk

    Syk, IC50:7.7 nM

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT02521376 Oncology PHASE1 COMPLETED 2017-10-25 Clinical Pharmacology of Miami... More >>, Inc. (CPMI), Miami, Florida, United States|Orlando Clinical Research Center, Orlando, Florida, United States|DaVita Clinical Research, Minneapolis, Minnesota, United States|The Texas Liver Institute, San Antonio, Texas, United States|APEX GmBH, Munich, Germany|Auckland Clinical Studies, Auckland, New Zealand Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.43mL

0.49mL

0.24mL

12.15mL

2.43mL

1.22mL

24.30mL

4.86mL

2.43mL

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