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Entospletinib

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Chemical compound Pharmaceutical compound
Entospletinib
Clinical data
Other namesGS-9973
Legal status
Legal status
  • Investigational
Identifiers
IUPAC name
  • 6-(1H-Indazol-6-yl)-N-(4-morpholin-4-ylphenyl)imidazopyrazin-8-amine
CAS Number
PubChem CID
DrugBank
UNII
KEGG
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC23H21N7O
Molar mass411.469 g·mol
3D model (JSmol)
SMILES
  • c1cn2cc(-c3ccc4cnc4c3)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

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). It has entered clinical trials for acute myeloid leukaemia (AML), chronic lymphocytic leukemia (CLL), diffuse large B cell lymphoma (DLBCL), graft-versus-host disease (GvHD), hematological malignancies, mantle cell lymphoma (MCL), and non-Hodgkin lymphoma (NHL).

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. Archived from the original on 2018-10-30. Retrieved 2018-10-30.
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