CC-99677 | MAPKAPK2 (MK2) inhibitor | Probechem Biochemicals

Chemical Structure : CC-99677

CAS No.: 1887069-10-4

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CC-99677 (Gamcemetinib, CC99677, BMS-986371)

货号: PC-21906Not For Human Use, Lab Use Only.

CC-99677 (Gamcemetinib, BMS-986371) is a potent, selective, covalent and orally bioavailable MAPKAPK2 (MK2) inhibitor with IC50 of 156.3 nM, potently inhibits HSP27 phosphorylation (pHSP27) with EC50 of 89 nM.

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5 mg	￥2580	In stock
10 mg	￥3980	In stock
25 mg	￥5980	In stock
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100 mg		Get quote

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生物&药学活性

CC-99677 (Gamcemetinib, BMS-986371) is a potent, selective, covalent and orally bioavailable MAPKAPK2 (MK2) inhibitor with IC50 of 156.3 nM, potently inhibits HSP27 phosphorylation (pHSP27) with EC50 of 89 nM.
CC-99677 covalently binds MK2 with Ki of 171.7 nM.
CC-99677 potently inhibits TNFα and GM-CSF (IC50=67 nM, 258 nM, respectively) and moderately inhibits IL-6 (IC50=865 nM) in LPS-stimulated PBMCs.
CC-99677 (20 & 100 mg/kg CC-99677 PO) inhibits paw swelling in a rat model of ankylosing spondylitis (AS), shows favorable safety in healthy human subjects in clinical investigations.

物理化学性质&存储条件

分子量	469.94
分子式	C22H20ClN5O3S
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	8H-[1,4]Diazepino[5',6':4,5]thieno[3,2-f]quinolin-8-one, 3-[[2-chloro-5-(ethoxymethyl)-4-pyrimidinyl]oxy]-9,10,11,12-tetrahydro-10-methyl-, (10R)-

参考文献

1. Malona J, et al. Transl Res. 2022 Nov;249:49-73.

CC-99677 (Gamcemetinib, CC99677, BMS-986371)

生物&药学活性

物理化学性质&存储条件

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CC-99677 (Gamcemetinib, CC99677, BMS-986371)

生物&药学活性

物理化学性质&存储条件

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