Entospletinib (GS-9973)
- CAS NO.:1229208-44-9
- Empirical Formula: C23H21N7O
- Molecular Weight: 411.46
- MDL number: MFCD28099806
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-07-02 08:55:41
What is Entospletinib (GS-9973)?
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.
The Uses of Entospletinib (GS-9973)
GS 9973 is a selective and orally bioavailable inhibitor of spleen tyrosine kinase (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.
Properties of Entospletinib (GS-9973)
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 |
Safety information for Entospletinib (GS-9973)
Computed Descriptors for Entospletinib (GS-9973)
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