Entospletinib

Entospletinib is an experimental drug for the treatment of various types of cancer under development by Gilead Sciences. It is an inhibitor of spleen tyrosine kinase (Syk).[1] It has entered clinical trials for acute myeloid leukaemia (AML), chronic lymphocytic leukemia (CLL),[2] diffuse large B cell lymphoma (DLBCL), graft-versus-host disease (GvHD), hematological malignancies, mantle cell lymphoma (MCL), and non-Hodgkin lymphoma (NHL).[3]

Entospletinib
Clinical data
Other namesGS-9973
Legal status
Legal status
  • Investigational
Identifiers
IUPAC name
  • 6-(1H-Indazol-6-yl)-N-(4-morpholin-4-ylphenyl)imidazo[1,2-a]pyrazin-8-amine
CAS Number
PubChem CID
DrugBank
UNII
KEGG
Chemical and physical data
FormulaC23H21N7O
Molar mass411.469 g·mol−1
3D model (JSmol)
SMILES
  • c1cn2cc(-c3ccc4cn[nH]c4c3)nc(Nc3ccc(N4CCOCC4)cc3)c2n1
InChI
  • 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)
  • Key:XSMSNFMDVXXHGJ-UHFFFAOYSA-N

References
  1. "Definition of entospletinib". NCI Cancer Dictionary. National Cancer Institute.
  2. Sharman J, Di Paolo J (June 2016). "Targeting B-cell receptor signaling kinases in chronic lymphocytic leukemia: the promise of entospletinib". Therapeutic Advances in Hematology. 7 (3): 157–70. doi:10.1177/2040620716636542. PMC 4872176. PMID 27247756.
  3. "Entospletinib - Gilead Sciences". Adis Insight.
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