Entospletinib | Syk inhibitor | Probechem Biochemicals

Chemical Structure : Entospletinib

CAS No.: 1229208-44-9

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Entospletinib (GS-9973)

货号: PC-73180Not For Human Use, Lab Use Only.

Entospletinib (GS-9973) is a potent, selective and orally bioavailable Syk kinase inhibitor with IC50 of 7.7 nM.

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25 mg	￥1480	In stock
50 mg	￥2380	In stock
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生物&药学活性

Entospletinib (GS-9973) is a potent, selective and orally bioavailable Syk kinase inhibitor with IC50 of 7.7 nM.
Entospletinib (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.
Entospletinib (GS-9973) combined with Idelalisib synergistically inhibits CLL cell viability and further disrupts chemokine signaling.
Entospletinib (GS-9973) (1-10 mg/kg, p.o.) significantly inhibits ankle inflammation in a rat collagen-induced arthritis model, inhibits pannus formation, cartilage damage, bone resorption, and peritosteal bone formation with ED50 of 1.2-3.9 mg/kg.

物理化学性质&存储条件

分子量	411.46
分子式	C23H21N7O
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	6-(1H-indazol-6-yl)-N-(4-morpholinophenyl)imidazo[1,2-a]pyrazin-8-amine

参考文献

1. Currie KS, et al. J Med Chem. 2014 May 8;57(9):3856-73.

2. Burke RT, et al. Oncotarget. 2014 Feb 28;5(4):908-15.

Entospletinib (GS-9973)

生物&药学活性

物理化学性质&存储条件

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Entospletinib (GS-9973)

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