ND2158 |CAS:1388896-07-8 Probechem Biochemicals

Chemical Structure : ND2158

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ND2158 (ND-2158, ND 2158)

货号: PC-38157Not For Human Use, Lab Use Only.

ND2158 (ND-2158) is a highly potent and selective IRAK4 inhibitor with IC50 of 1.3 nM.

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生物&药学活性

ND2158 (ND-2158) is a highly potent and selective IRAK4 inhibitor with IC50 of 1.3 nM.
ND2158 demonstrates high selectivity against 334 kinases, and >1000-fold over IRAK1.
ND2158 blocked TNF production, collagen-induced arthritis, and gout formation in mice, suppressed LPS-induced TNF production, alleviated collagen-induced arthritis, and blocked gout formation in mouse models.
IRAK4 inhibition promoted killing of ABC DLBCL lines harboring MYD88 L265P, by down-modulating survival signals, including NF-κB and autocrine IL-6/IL-10 engagement of the JAK-STAT3 pathway.
In ABC DLBCL xenograft models, IRAK4 inhibition suppressed tumor growth as a single agent, and in combination with the Bruton's tyrosine kinase (BTK) inhibitor ibrutinib or the Bcl-2 inhibitor ABT-199.

物理化学性质&存储条件

分子量	446.566
分子式	C22H30N4O4S
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	(S)-2-hydroxy-3-((R)-4-(((1r,4R)-4-morpholinocyclohexyl)oxy)-6,7-dihydro-5H-cyclopenta[4,5]thieno[2,3-d]pyrimidin-5-yl)propanamide

参考文献

1. Priscilla N Kelly, et al. J Exp Med. 2015 Dec 14;212(13):2189-201.

2. Giménez N, et al. Leukemia. 2020 Jan;34(1):100-114.

ND2158 (ND-2158, ND 2158)

生物&药学活性

物理化学性质&存储条件

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ND2158 (ND-2158, ND 2158)

生物&药学活性

物理化学性质&存储条件

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