A selective spleen tyrosine kinase inhibitor
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GS-9973

Item No. 17653

Technical Information
Formal Name
6-(1H-indazol-6-yl)-N-[4-(4-morpholinyl)phenyl]-imidazo[1,2-a]pyrazin-8-amine
CAS Number
1229208-44-9
Molecular Formula
C23H21N7O
Formula Weight
Purity
≥95%
A crystalline solid
DMF: 10 mg/mlDMSO: 15 mg/mlDMSO:PBS(pH 7.2) (1:2): 0.3 mg/ml
λmax
244, 328 nm
SMILES
C12=NC=CN1C=C(C3=CC=C(C=NN4)C4=C3)N=C2NC5=CC=C(N6CCOCC6)C=C5
InChi Code
InChI=1S/C23H21N7O/c1-2-17-14-25-28-20(17)13-16(1)21-15-30-8-7-24-23(30)22(27-21)26-18-3-5-19(6-4-18)29-9-11-31-12-10-29/h1-8,13-15H,9-12H2,(H,25,28)(H,26,27)
InChi Key
XSMSNFMDVXXHGJ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    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.1 In conjunction with the PI3Kδ inhibitor CAL-101 (Item No. 15279), it has been used to reduce chronic lymphocytic leukemia cell survival and to disrupt chemokine signaling at nanomolar concentrations.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Currie, K.S., Kropf, J.E., Lee, T., et alDiscovery of GS-9973, a selective and orally efficacious inhibitor of spleen tyrosine kinase. J. Med. Chem. 57(9), 3856-3873 (2014).

    2. Burke, R.T., Meadows, S., Loriaux, M.M., et alA potential therapeutic strategy for chronic lymphocytic leukemia by combining Idelalisib and GS-9973, a novel spleen tyrosine kinase (Syk) inhibitor. Oncotarget 5(4), 908-915 (2014).