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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-MEKK (MAP3K)-Tilpisertib
Tilpisertib

Chemical Structure : Tilpisertib

CAS No.: 2065153-41-3

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Tilpisertib (GS-4875, GS4875)

货号: PC-38374Not For Human Use, Lab Use Only.

Tilpisertib (GS-4875) is a potent, highly selective TPL2 kinase (COT, MAP3K8) inhibitor with IC50 of 1.3 nM, with no significant off-target binding activity.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Tilpisertib (GS-4875) is a potent, highly selective TPL2 kinase (COT, MAP3K8) inhibitor with IC50 of 1.3 nM, with no significant off-target binding activity.
Tilpisertib (GS-4875) selectively inhibited LPS and TNFα-stimulated phosphorylation of TPL2, MEK, and ERK, with little to no inhibition of phosphorylated p38, JNK or p65.
Tilpisertib (GS-4875) similarly inhibited in the RNA production and secretion of TNFα, IL-1β, IL-6, and IL-8 following LPS stimulation in primary human monocytes.
Tilpisertib (GS-4875) inhibited the secretion of TNFα and IL-6 following LPS stimulation in monocyte-derived dendritic cells.
Tilpisertib (GS-4875) reduced TNFα-stimulated pERK with no effect on ERK activation downstream of EGF in A431 cells stimulated with either TNFα or EGF.
Tilpisertib (GS-4875) treatment showed dose and exposure dependent inhibition (IC50=667 nM) of LPS-stimulated TNFα production a rat LPS-TNFα model of acute inflammation.

物理化学性质&存储条件

分子量 593.132
分子式 C33H33ClN8O
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)-6-(((1-(bicyclo[1.1.1]pentan-1-yl)-1H-1,2,3-triazol-4-yl)(2-methyl-1-oxo-1,2-dihydroisoquinolin-5-yl)methyl)amino)-8-chloro-4-(neopentylamino)quinoline-3-carbonitrile

参考文献

1. Matthew Warr, et al. Meeting: 2019 ACR/ARP Annual Meeting.

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