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Chemical Structure : CC-99677
CAS No.: 1887069-10-4
Catalog No.: 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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 2 mg | $458 | In stock | |
| 5 mg | $758 | In stock | |
| 10 mg | Get quote | ||
| 25 mg | Get quote | ||
| 100 mg | Get quote |
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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.
| M.Wt | 469.94 | |
| Formula | C22H20ClN5O3S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| 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)- |
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1. Malona J, et al. Transl Res. 2022 Nov;249:49-73.
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