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
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
N-Bromosuccinimide Price
- Product number
- 17653
- Product name
- GS-9973
- Purity
- ≥95%
- Packaging
- 1mg
- Price
- $36
- Updated
- 2024/03/01
- Product number
- 17653
- Product name
- GS-9973
- Purity
- ≥95%
- Packaging
- 5mg
- Price
- $105
- Updated
- 2024/03/01
- Product number
- 17653
- Product name
- GS-9973
- Purity
- ≥95%
- Packaging
- 10mg
- Price
- $172
- Updated
- 2024/03/01
- Product number
- 17653
- Product name
- GS-9973
- Purity
- ≥95%
- Packaging
- 50mg
- Price
- $341
- Updated
- 2024/03/01
- Product number
- G797250
- Product name
- GS9973
- Packaging
- 5mg
- Price
- $85
- Updated
- 2021/12/16
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.
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View Lastest Price from Entospletinib (GS-9973) manufacturers
- 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