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Entospletinib

Entospletinib structure

CAS No:
1229208-44-9
Formula:
C23H21N7O
Chemical Name:
Entospletinib
Synonyms:
Imidazo[1,2-a]pyrazin-8-amine,6-(1H-indazol-6-yl)-N-[4-(4-morpholinyl)phenyl]-;6-(1H-Indazol-6-yl)-N-[4-(4-morpholinyl)phenyl]imidazo[1,2-a]pyrazin-8-amine;GS 9973;Entospletinib
Categories:
Biochemical Engineering > Inhibitors

Description

Entospletinib (GS-9973) is an orally bioavailable, selective Syk inhibitor with IC50 of 7.7 nM in a cell-free assay and showed 13-to >1000-fold cellular selectivity for Syk over other kinases(including Jak2, ckit, Flt3, Ret, KDR) as assessed by target protein phosphorylation or functional response.

Entospletinib has been used in trials studying the treatment of Oncology, Follicular Lymphoma, B-cell Malignancies, Mantle Cell Lymphoma, and Non-Hodgkin Lymphoma, among others.|Entospletinib is an orally available inhibitor of spleen tyrosine kinase (Syk), with potential antineoplastic activity. Upon oral administration of entospletinib, this agent may inhibit the activity of Syk, which inhibits B-cell receptor (BCR) signaling and leads to an inhibition of tumor cell activation, migration, adhesion and proliferation. Syk, a non-receptor cytoplasmic, BCR-associated tyrosine kinase, is expressed in hematopoietic tissues and is often overexpressed in hematopoeitic malignancies.

Entospletinib Basic Attributes

Molecular Weight：

411.45914

Exact Mass：

411.46

EC Number：

-0

UNII：

6I3O3W6O3B

NCI Thesaurus Code：

C105402

Characteristics

PSA：

83.4

XLogP3：

3.6

Density：

1.45±0.1 g/cm3(Predicted)

Refractive Index：

1.772

Water Solubility：

H2O: Practically insoluble (0.045 g/L) (25 ºC)

Drug Information

Drug Indication：

Treatment of acute myeloid leukaemia

MeSH Entry Terms：

6-(1H-indazol-6-yl)-N-(4-morpholinophenyl)imidazo(1,2-a)pyrazin-8-amine

Entospletinib Use and Manufacturing

Use Classification：

Human drugs -> Rare disease (orphan)|Human Drugs -> EU pediatric investigation plans

Computed Properties

Molecular Weight:411.5
XLogP3:3.6
Hydrogen Bond Donor Count:2
Hydrogen Bond Acceptor Count:6
Rotatable Bond Count:4
Exact Mass:411.18075832
Monoisotopic Mass:411.18075832
Topological Polar Surface Area:83.4
Heavy Atom Count:31
Complexity:595
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

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Entospletinib

CAS No.: 1229208-44-9

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