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GS-9973

Cat. No. M2729
GS-9973 Structure
Synonym:

Entospletinib

Size Price Availability Quantity
10mg USD 110  USD110 In stock
50mg USD 330  USD330 In stock
100mg USD 530  USD530 In stock
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Quality Control & Documentation
Biological Activity

GS-9973 is an orally bioavailable, selective Syk inhibitor with IC50 of 7.7 nM, which is currently undergoing clinical evaluation for autoimmune and oncology indications.

Chemical Information
Molecular Weight 411.46
Formula C23H21N7O
CAS Number 1229208-44-9
Solubility (25°C) DMSO 60 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Silpa Narayanan, et al. The Spleen Tyrosine Kinase Inhibitor, Entospletinib (GS-9973) Restores Chemosensitivity in Lung Cancer Cells by Modulating ABCG2-mediated Multidrug Resistance

[2] Anjali Cremer, et al. Resistance Mechanisms to SYK Inhibition in Acute Myeloid Leukemia

[3] Chen Qu, et al. Tyrosine kinase SYK is a potential therapeutic target for liver fibrosis

[4] Ana Colado, et al. The kinase inhibitors R406 and GS-9973 impair T cell functions and macrophage-mediated anti-tumor activity of rituximab in chronic lymphocytic leukemia patients

[5] Kevin S Currie, et al. Discovery of GS-9973, a selective and orally efficacious inhibitor of spleen tyrosine kinase

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  Catalog
Abmole Inhibitor Catalog




Keywords: GS-9973, Entospletinib supplier, Syk, inhibitors, activators


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