ChemicalBook > CAS DataBase List > MK-8353
MK-8353
MK-8353
- CAS No.1184173-73-6
- Chemical Name:MK-8353
- CBNumber:CB34668195
- Molecular Formula:C37H41N9O3S
- Formula Weight:691.84
- MOL File:1184173-73-6.mol
MK-8353 Property
- Density 1.36±0.1 g/cm3(Predicted)
- storage temp. 2-8°C
- solubility Soluble in DMSO
- pka 11.89±0.40(Predicted)
- form Solid
- color Off-white to light brown
-
Symbol(GHS)
- Signal wordWarning
- Hazard statements H302-H315-H319-H335
- Precautionary statements P261-P305+P351+P338
MK-8353 Chemical Properties,Usage,Production
- Uses MK-8353 (SCH900353) is a potent, selective and orally available ERK1/2 inhibitor, with IC50s of 23.0 nM and 8.8 nM, respectively; MK-8353 has antitumor activity.
- Definition ChEBI: MK-8353 is a member of the class of indazoles that is 1H-indazole substituted by a 6-(propan-2-yloxy)pyridin-3-yl group at position 3 and by a {[(3S)-3-(methylsulfanyl)-1-(2-{4-[4-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl]-3,6-dihydropyridin-1(2H)-yl}-2-oxoethyl)pyrrolidin-3-yl]carbonyl}amino group at position 5. It is a potent and selective inhibitor of ERK1 and ERK2 in vitro (IC50 values of 23.0 nM and 8.8 nM, respectively). The drug is being developed by Merck Sharp & Dohme and is currently in clinical development for the treatment of advanced/metastatic solid tumors. It has a role as an EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor, an antineoplastic agent and an apoptosis inducer. It is a member of indazoles, a member of triazoles, a dihydropyridine, a member of pyridines, an aromatic ether, a secondary carboxamide, a pyrrolidinecarboxamide, a N-alkylpyrrolidine, a methyl sulfide and a tertiary carboxamide.
-
in vivo
MK-8353 (60 mg/kg, p.o., bid (twice daily)) causes at least 50% tumor growth inhibition or regression in 83% of the animal models bearing different tumor cells, including LOX, Colo-205, MIA PaCa-2, and Calu-6 cells[1].
- IC 50 ERK2: 8.8 nM (IC50); ERK1: 23 nM (IC50)
- References [1] Moschos SJ, et al. Development of MK-8353, an orally administered ERK1/2 inhibitor, in patients with advanced solid tumors. JCI Insight. 2018 Feb 22;3(4). pii: 92352. DOI:10.1172/jci.insight.92352
MK-8353 Preparation Products And Raw materials
Raw materials
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1184173-73-6, MK-8353Related Search:
- 合成材料中间体
- 合成有机化合物配体
- 抑制剂
- C37H41N9O3S
- 化合物MK-8353,10 MM DMSO 溶液
- (S)-N-(3-(6-异丙氧基吡啶-3-基)-1H-吲唑-5-基)-1-(2-(4-(4-(1-甲基-1H-1,2,4-三唑-3-基)苯基)-5,6-二氢吡啶-1(2H)- 基)-2-氧代乙基)-3-(甲硫基)吡咯烷-3-甲酰胺
- 化合物MK-8353
- 化合物 T12069
- (3S)-1-[2-[3,6-二氢-4-[4-(1-甲基-1H-1,2,4-三唑-3-基)苯基]-1(2H)-吡啶基]-2-氧代乙基]-N-[3-[6-(1-甲基乙氧基)-3-吡啶基]-1H-吲唑-5-基]-3-(甲硫基)-3-吡咯烷甲酰胺
- 1184173-73-6
- MK-8353, 10 mM in DMSO
- SCH900353 (MK-8353)
- (S)-N-(3-(6-Isopropoxypyridin-3-yl)-1H-indazol-5-yl)-1-(2-(4-(4-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)-3,6-dihydropyridin-1(2H)-yl)-2-oxoethyl)-3-(methylthio)pyrrolidine-3-carboxamide
- SCH 900353,Extracellular signal regulated kinases,Inhibitor,inhibit,MK 8353,SCH-900353,MK-8353,ERK,MK8353
- 3-Pyrrolidinecarboxamide, 1-[2-[3,6-dihydro-4-[4-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl]-1(2H)-pyridinyl]-2-oxoethyl]-N-[3-[6-(1-methylethoxy)-3-pyridinyl]-1H-indazol-5-yl]-3-(methylthio)-, (3S)-
- MK-8353 (SCH900353)
- SCH900353
- SCH-900565
- MK-8353