Description Features In vitro In vivo
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Entospletinib (GS-9973)

Description Features In vitro In vivo
Product Name
Entospletinib (GS-9973)
CAS No.
1229208-44-9
Chemical Name
Entospletinib (GS-9973)
Synonyms
Entospletinib;6-(1H-indazol-6-yl)-N-(4-morpholinophenyl)imidazo[1,2-a]pyrazin-8-amine;GS-9973;CS-1602;GS-9973;GS 9973;GS-9973, Entospletinib;Entospletinib (GS-9973);Entospletinib Dimesylate;Entospletinib, 10 mM in DMSO;GS9973; GS 9973; ENTOSPLETINIB
CBNumber
CB92703799
Molecular Formula
C23H21N7O
Formula Weight
411.46
MOL File
1229208-44-9.mol
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Entospletinib (GS-9973) Property

Density 
1.45±0.1 g/cm3(Predicted)
storage temp. 
Desiccate at -20°C
solubility 
insoluble in EtOH; insoluble in H2O; ≥20.55 mg/mL in DMSO
form 
solid
pka
12.54±0.40(Predicted)
color 
White to gray
InChI
InChI=1S/C23H21N7O/c1-2-17-14-25-28-20(17)13-16(1)21-15-30-8-7-24-23(30)22(27-21)26-18-3-5-19(6-4-18)29-9-11-31-12-10-29/h1-8,13-15H,9-12H2,(H,25,28)(H,26,27)
InChIKey
XSMSNFMDVXXHGJ-UHFFFAOYSA-N
SMILES
C12=NC=CN1C=C(C1=CC3=C(C=C1)C=NN3)N=C2NC1=CC=C(N2CCOCC2)C=C1
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Cayman Chemical
Product number
17653
Product name
GS-9973
Purity
≥95%
Packaging
1mg
Price
$36
Updated
2024/03/01
Cayman Chemical
Product number
17653
Product name
GS-9973
Purity
≥95%
Packaging
5mg
Price
$105
Updated
2024/03/01
Cayman Chemical
Product number
17653
Product name
GS-9973
Purity
≥95%
Packaging
10mg
Price
$172
Updated
2024/03/01
Cayman Chemical
Product number
17653
Product name
GS-9973
Purity
≥95%
Packaging
50mg
Price
$341
Updated
2024/03/01
Usbiological
Product number
451449
Product name
GS 9973
Packaging
1mg
Price
$319
Updated
2021/12/16
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Entospletinib (GS-9973) Chemical Properties,Usage,Production

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.

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. The combination of idelalisib and GS-9973 synergistically inhibits CLL cell viability and further disrupts chemokine signaling.

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 .

Description

Spleen 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 , it has been used to reduce chronic lymphocytic leukemia cell survival and to disrupt chemokine signaling at nanomolar concentrations.

Uses

GS 9973 is a selective and orally bioavailable inhibitor of spleen tyrosine kinase (Syk).

in vivo

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

target

Syk

References

[1]. currie ks, kropf je, lee t, et al. discovery of gs-9973, a selective and orally efficacious inhibitor of spleen tyrosine kinase. j med chem, 2014, 57(9): 3856-3873.
[2]. burke rt1, meadows s, loriaux mm, 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, 5(4): 908-915.
[3]. sharman j, hawkins m, kolibaba k, et al. an open-label phase 2 trial of entospletinib (gs-9973), a selective spleen tyrosine kinase inhibitor, in chronic lymphocytic leukemia. blood, 2015, 125(15): 2336-2343.

Entospletinib (GS-9973) Preparation Products And Raw materials

Raw materials

Preparation Products

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Entospletinib (GS-9973) Suppliers

China 133 India 2 United States 17 Global 152
Shanghai joygo pharmacetical tech., Co., Ltd.
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(86) 21-58955996
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Bide Pharmatech Ltd.
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AdooQ Bioscience CHINA
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View Lastest Price from Entospletinib (GS-9973) manufacturers

Career Henan Chemical Co
Product
Entospletinib (GS-9973) 1229208-44-9
Price
US $6.68/KG
Min. Order
1KG
Purity
97%-99%
Supply Ability
1kg-1000kg
Release date
2020-01-08

1229208-44-9, Entospletinib (GS-9973)Related Search:

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  • GS-9973
  • Entospletinib
  • 6-(1H-Indazol-6-yl)-N-[4-(4-morpholinyl)phenyl]imidazo[1,2-a]pyrazin-8-amine
  • GS-9973;GS 9973
  • CS-1602
  • GS9973; GS 9973; ENTOSPLETINIB
  • 6-(1H-indazol-6-yl)-N-(4-morpholinophenyl)imidazo[1,2-a]pyrazin-8-amine
  • Entospletinib (GS-9973)
  • Entospletinib Dimesylate
  • 6-(1H-indazol-6-yl)-N-(4-morpholin-4-ylphenyl)imidazo[1,2-a]pyrazin-8-amine
  • GS-9973, Entospletinib
  • 6-(1H-INDAZOL-6-YL)-N-(4-MORPHOLINOPHENYL)IMIDAZO[1,2-A]PYRAZIN-8-AMINE，GS-9973
  • Imidazo[1,2-a]pyrazin-8-amine, 6-(1H-indazol-6-yl)-N-[4-(4-morpholinyl)phenyl]-
  • Entospletinib (GS-9973) USP/EP/BP
  • Entospletinib, 10 mM in DMSO
  • Entospletinib (GS-9973) ，S7523
  • 1229208-44-9
  • Inhibitors