GS-9973 free base · Synonyms: Entospletinib

Entospletinib is an orally bioavailable, selective Syk inhibitor.

For research use only. Not for human or veterinary use.

Target Syk

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

GS-9973 structure

CAS No.: 1229208-44-9

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
250 mg	USD 480.00	BP-02487-250mg	In stock	Get quote
500 mg	USD 770.00	BP-02487-500mg	In stock	Get quote
1 g	USD 1,230.00	BP-02487-1g	In stock	Get quote
2 g	USD 1,960.00	BP-02487-2g	In stock	Get quote
3 g	USD 2,360.00	BP-02487-3g	In stock	Get quote
5 g	USD 3,145.00	BP-02487-5g	In stock	Get quote
10 g	USD 5,030.00	BP-02487-10g	In stock	Get quote

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Description

Entospletinib (GS-9973) is an orally bioavailable, selective Syk inhibitor with an IC50 of 7.7 nM.

Biological activity

In Vitro Entospletinib (GS-9973) shows good bidirectional permeability across Caco-2 cell monolayers in vitro. In cells, Entospletinib (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 Entospletinib (GS-9973) synergistically inhibits CLL cell viability and further disrupts chemokine signaling. 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.

Identifiers

SMILES: C1CN(CCO1)C1=CC=C(NC2=NC(=CN3C=CN=C23)C2=CC3=C(C=NN3)C=C2)C=C1
InChIKey: XSMSNFMDVXXHGJ-UHFFFAOYSA-N

Specifications

MW (average): 411.4591
Formula: C₂₃H₂₁N₇O
CAS No.: 1229208-44-9
Physical state: Solid
Color: White to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20°C, 3 years , 4°C, 2 years ; In solvent -20°C, 1 year;

Solubility

Soluble in DMSO

Documents

References

[1].Currie KS, et al. Discovery of GS-9973, a Selective and Orally Efficacious Inhibitor of Spleen Tyrosine Kinase. J Med Chem. 2014 May 8;57(9):3856-73.

[2].Burke RT, 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 Feb 28;5(4):908-15.

Same research area

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