GS-9973 (ENTOSPLETINIB)

Background Information:

Spleen tyrosine kinase (Syk), a non-receptor cytoplasmic,
BCR-associated enzyme, is expressed in hematopoietic tissues and is
often overexpressed in hematopoeitic malignancies. GS-9973
(Entospletinib) is a highly selective and orally efficacious inhibitor
of spleen tyrosine kinase (Syk) with an IC50 of 7.7 nM. It inhibits the
activity of Syk, which inhibits B-cell receptor (BCR) signaling and
leads to an inhibition of tumor cell activation, migration, adhesion and
proliferation. It is currently in clinical evaluation for autoimmune
and oncology indications.

Reference:

1. K. S. Currie, et al., Discovery of GS-9973, a Selective and Orally
Efficacious Inhibitor of Spleen Tyrosine Kinase, J. Med. Chem., April
6, 2014.

APIM050160: GS-9973 (ENTOSPLETINIB)

CAS No.: 1229208-44-9.
Molecular Formula: C₂₃H₂₁N₇O.
Molecular Weight: 411.5.
Purity: >99% Purity (HPLC, detected at 214 and 254 nm).
QC: HPLC-MS, ¹HNMR, and Quantitative Elemental Analysis.
Solubility: Soluble in DMSO.
Storage: Store at 0°C (short term), -20°C (long term), desiccated.