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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-MAPKAPK2 (MK2)-PF-3644022
PF-3644022

Chemical Structure : PF-3644022

CAS No.: 1276121-88-0

PF-3644022 (PF 3644022;PF3644022)

货号: PC-70143Not For Human Use, Lab Use Only.

PF-3644022 is a potent and selective, freely reversible, ATP-competitive inhibitor of MAPKAP2 (MK2) with Ki of 3 nM.

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5 mg ¥2480 In stock
10 mg ¥3980 In stock
25 mg ¥5880 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

PF-3644022 is a potent and selective, freely reversible, ATP-competitive inhibitor of MAPKAP2 (MK2) with Ki of 3 nM.
PF-3644022 shows good selectivity against a panel of 200 human kinases.
PF-3644022 potently inhibits TNFα production with similar activity (IC50=160 nM) in U937 cells and hPBMCs, blocks TNFα and IL-6 production in LPS-stimulated human whole blood with IC50 of 1.6 and 10.3 uM, respectively.
PF-3644022 is activite in the rat LPS-induced TNFalpha model and orally efficacious.

物理化学性质&存储条件

分子量 374.46
分子式 C21H18N4OS
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

100 mM in DMSO (37.4 mg/mL)

Chemical Name/SMILES

(10R)-9,10,11,12-Tetrahydro-10-methyl-3-(6-methyl-3-pyridinyl)-8H-[1,4]diazepino[5',6':4,5]thieno[3,2-f]quinolin-8-one

参考文献

1. Mourey RJ, et al. J Pharmacol Exp Ther. 2010 Jun;333(3):797-807.

2. Song H, et al. Am J Transl Res. 2015 Nov 15;7(11):2355-63.

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