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;GS9973; GS 9973; ENTOSPLETINIB;Entospletinib (GS-9973) USP/EP/BP
- CBNumber:
- CB92703799
- Molecular Formula:
- C23H21N7O
- Molecular Weight:
- 411.46
- MDL Number:
- MFCD28099806
- MOL File:
- 1229208-44-9.mol
| 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) |
| FDA UNII | 6I3O3W6O3B |
| NCI Drug Dictionary | entospletinib |
Entospletinib (GS-9973) price More Price(22)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 17653 | GS-9973 ≥95% | 1229208-44-9 | 1mg | $36 | 2024-03-01 | Buy |
| Cayman Chemical | 17653 | GS-9973 ≥95% | 1229208-44-9 | 5mg | $105 | 2024-03-01 | Buy |
| Cayman Chemical | 17653 | GS-9973 ≥95% | 1229208-44-9 | 10mg | $172 | 2024-03-01 | Buy |
| Cayman Chemical | 17653 | GS-9973 ≥95% | 1229208-44-9 | 50mg | $341 | 2024-03-01 | Buy |
| Usbiological | 451449 | GS 9973 | 1229208-44-9 | 1mg | $319 | 2021-12-16 | Buy |
Entospletinib (GS-9973) Chemical Properties,Uses,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).
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
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32480 | 60 |
| Hubei Jusheng Technology Co.,Ltd. | 18871490254 | linda@hubeijusheng.com | CHINA | 28180 | 58 |
| BOC Sciences | +1-631-485-4226 | inquiry@bocsci.com | United States | 19553 | 58 |
| career henan chemical co | +86-0371-86658258 15093356674; | factory@coreychem.com | China | 29826 | 58 |
| HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6313 | 58 |
| Dideu Industries Group Limited | +86-29-89586680 +86-15129568250 | 1026@dideu.com | China | 29220 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10523 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
| Coresyn Pharmatech Co., Ltd. | +86-571-86626709 +86-18157142896 | cbc@coresyn.com | China | 9991 | 58 |
| Nantong HI-FUTURE Biology Co., Ltd. | +undefined18051384581 | sales@chemhifuture.com | China | 3136 | 58 |
View Lastest Price from Entospletinib (GS-9973) manufacturers
| Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
|---|---|---|---|---|---|---|---|---|
 |
2020-01-09 | Entospletinib (GS-9973)
1229208-44-9
|
US $6.68 / KG | 1KG | 97%-99% | 1kg-1000kg | Career Henan Chemical Co |
-
- Entospletinib (GS-9973)
1229208-44-9
- US $6.68 / KG
- 97%-99%
- Career Henan Chemical Co