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Entospletinib (GS-9973)

Entospletinib (GS-9973) Suppliers list
Company Name: ATK CHEMICAL COMPANY LIMITED
Tel: 21-51619050
Email: ivan@atkchemical.com
Products Intro: Product Name:GS-9973
CAS:1229208-44-9
Purity:98% HPLC Package:5MG;10MG;50MG;100MG,1G,5G
Company Name: Hubei Jusheng Technology Co.,Ltd.
Tel: 86-18871470254
Email: linda@hubeijusheng.com
Products Intro: Product Name:Entospletinib (GS-9973)
CAS:1229208-44-9
Purity:0.99 Package:5KG;1KG
Company Name: career henan chemical co
Tel: +86-0371-86658258
Email: factory@coreychem.com
Products Intro: Product Name:Entospletinib (GS-9973)
CAS:1229208-44-9
Purity:97%-99% Package:1KG;6.68USD
Company Name: TargetMol Chemicals Inc.
Tel: +1-781-999-5354 +1-00000000000
Email: marketing@targetmol.com
Products Intro: Product Name:Entospletinib;GS-9973
CAS:1229208-44-9
Purity:99.51% Package:5 mg;10 mg;50 mg;100 mg;200 mg;1 mL * 10 mM (in DMSO);2 mg Remarks:REAGENT;FOR LABORATORY USE ONLY
Company Name: HANGZHOU CLAP TECHNOLOGY CO.,LTD
Tel: 86-571-88216897、88216896 13588875226
Email: sales@hzclap.com
Products Intro: Product Name:Entospletinib
CAS:1229208-44-9
Purity:38099% Package:10kg 25kg 200 kilograms per barrel Remarks:good

Entospletinib (GS-9973) manufacturers

  • Entospletinib (GS-9973)
  • $6.68 / 1KG
  • 2020-01-09
  • CAS:1229208-44-9
  • Min. Order: 1KG
  • Purity: 97%-99%
  • Supply Ability: 1kg-1000kg
Entospletinib (GS-9973) Basic information
Description Features In vitro In vivo
Product Name:Entospletinib (GS-9973)
Synonyms:GS-9973;6-(1H-Indazol-6-yl)-N-[4-(4-morpholinyl)phenyl]imidazo[1,2-a]pyrazin-8-amine;Entospletinib (GS-9973);Entospletinib Dimesylate;GS-9973, Entospletinib;GS-9973;GS 9973;CS-1602;GS9973; GS 9973; ENTOSPLETINIB
CAS:1229208-44-9
MF:C23H21N7O
MW:411.46
EINECS:
Product Categories:Inhibitors
Mol File:1229208-44-9.mol
Entospletinib (GS-9973) Structure
Entospletinib (GS-9973) Chemical Properties
density 1.45±0.1 g/cm3(Predicted)
pka12.54±0.40(Predicted)
Safety Information
MSDS Information
Entospletinib (GS-9973) Usage And Synthesis
DescriptionEntospletinib (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.
FeaturesOrally bioavailable Syk-selective inhibitor that has been tested in Phase II clinical trials for treatment of Haematological Malignancies.
In vitroGS-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. The combination of idelalisib and GS-9973 synergistically inhibits CLL cell viability and further disrupts chemokine signaling.
In vivoGS-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 .
DescriptionSpleen tyrosine kinase (Syk) is a non-receptor tyrosine kinase that upon phosphorylation binds to immunoreceptor tyrosine-based activation motifs of FcRγ chains and mediates downstream signaling related to platelet function and inflammation. GS-9973 is a potent Syk inhibitor (IC50 = 7.7 nM) that demonstrates 10-35-fold selectivity for Syk over a panel of 359 nonmutant kinases. In conjunction with the PI3Kδ inhibitor CAL-101 (Item No. 15279), it has been used to reduce chronic lymphocytic leukemia cell survival and to disrupt chemokine signaling at nanomolar concentrations.
UsesGS 9973 is a selective and orally bioavailable inhibitor of spleen tyrosine kinase (Syk).
Entospletinib (GS-9973) Preparation Products And Raw materials
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