Synonym
CC-99677; CC 99677; CC99677; Gamcemetinib
IUPAC/Chemical Name
(10R)-3-[[2-Chloro-5-(ethoxymethyl)-4-pyrimidinyl]oxy]-9,10,11,12-tetrahydro-10-methyl-8H-[1,4]diazepino[5',6':4,5]thieno[3,2-f]quinolin-8-one
InChi Key
PYOQIOLRFIRRSO-LLVKDONJSA-N
InChi Code
InChI=1S/C22H20ClN5O3S/c1-3-30-10-12-9-25-22(23)28-21(12)31-16-7-4-13-14(27-16)5-6-15-17(13)18-19(32-15)20(29)26-11(2)8-24-18/h4-7,9,11,24H,3,8,10H2,1-2H3,(H,26,29)/t11-/m1/s1
SMILES Code
O=C1N[C@H](C)CNC2=C1SC3=CC=C4N=C(OC5=NC(Cl)=NC=C5COCC)C=CC4=C32
Purity
>97% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Inhibitors of p38 are associated with tachyphylaxis in patients with RA and other inflammatory diseases, where early reduction in ex vivo production of cytokines, such as TNF-α, or endogenous inflammatory markers, such as CRP, did not persist despite continued treatment. Thus, p38 inhibitors have not advanced in clinical development. Targets downstream of p38 have been identified to avoid these limitations. The mitogen-activated protein kinase-activated protein kinase-2 (MK2) pathway is activated downstream of p38, and activation of MK2 increases the stability and translation of mRNA of proinflammatory factors (e.g., TNF-α, IL-17, IL-6).
Preparing Stock Solutions
The following data is based on the
product
molecular weight
469.94
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
Schwarz, M., Kurkunov, M., Wittlinger, F., Rudalska, R., Wang, G., Schwalm, M. P., ... & Gehringer, M. (2024). Development of Highly Potent and Selective Covalent FGFR4 Inhibitors Based on SNAr Electrophiles. Journal of medicinal chemistry, 67(8), 6549-6569.
Hillebrand, L., Liang, X. J., Serafim, R. A., & Gehringer, M. (2024). Emerging and re-emerging warheads for targeted covalent inhibitors: an update. Journal of medicinal chemistry, 67(10), 7668-7758.
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Dahl, A. (2017). Rufinamide is an anticonvulsant medication Menu.
