[CAS NO. 1229208-44-9] Entospletinib (GS-9973)

Name: Entospletinib (GS-9973)
Brand: Arctom Scientific
SKU: SLK-S7523

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PRODUCTS SPECIFICATIONS [1229208-44-9]

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Catalog

SLK-S7523

Brand

Selleck

CAS

1229208-44-9

DESCRIPTION [1229208-44-9]

Overview

MDL	MFCD28099806
Molecular Weight	411.46
Molecular Formula	C23H21N7O
SMILES	N(C=1C=2N(C=C(N1)C=3C=C4C(=CC3)C=NN4)C=CN2)C5=CC=C(C=C5)N6CCOCC6

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.4304 mL	12.1518 mL	24.3037 mL
5 mM	0.4861 mL	2.4304 mL	4.8607 mL
10 mM	0.2430 mL	1.2152 mL	2.4304 mL
50 mM	0.0486 mL	0.2430 mL	0.4861 mL

Description

Entospletinib (GS-9973) is an orally bioavailable, selective inhibitor with 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.

Features

Orally bioavailable Syk-selective inhibitor that has been tested in Phase II clinical trials for treatment of Haematological Malignancies.

Targets

Syk ^[1]
(Cell-free assay)

7.7 nM

In vitro

GS-9973 shows good bidirectional permeability across Caco-2 cell monolayers in vitro. In cells, GS-9973 also shows excellent selectivity for Syk, and potently inhibits BCR-mediated activation and proliferation of B-cells as well as immune-complex-stimulated cytokine production in monocytes. The combination of idelalisib and GS-9973 synergistically inhibits CLL cell viability and further disrupts chemokine signaling.

In vivo

GS-9973 (1 mg/kg p.o.) shows moderate to high bioavailability in rat and dog. In a rat collagen-induced arthritis model, GS-9973 (1-10 mg/kg p.o.) significantly inhibits ankle inflammation. Moreover, GS-9973 also shows disease-modifying activity in multiple histological measurements, including inhibition of pannus formation, cartilage damage, bone resorption, and peritosteal bone formation with ED50 ranging from 1.2 to 3.9 mg/kg .

References

[1] J Med Chem. 2014, 57(9), 3856-3873.
[2] Burke RT, et al. Oncotarget. 2014, 5(4), 908-915.

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