MK-8353
- Product Name
- MK-8353
- CAS No.
- 1184173-73-6
- Chemical Name
- MK-8353
- Synonyms
- MK-8353;SCH900353;SCH-900565;MK-8353 (SCH900353);SCH900353 (MK-8353);MK-8353, 10 mM in DMSO;SCH 900353,Extracellular signal regulated kinases,Inhibitor,inhibit,MK 8353,SCH-900353,MK-8353,ERK,MK8353;(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;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)-
- 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
- InChIKey
- KPQQGHGDBBJGFA-QNGWXLTQSA-N
- SMILES
- N1(CC(N2CCC(C3=CC=C(C4N=CN(C)N=4)C=C3)=CC2)=O)CC[C@@](SC)(C(NC2C=CC3=C(C=2)C(C2=CC=C(OC(C)C)N=C2)=NN3)=O)C1
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- BISN0200
- Product name
- MK-8353
- Packaging
- 2mg
- Price
- $149
- Updated
- 2021/12/16
- Product number
- CS-0040548
- Product name
- MK-8353
- Purity
- 98.79%
- Packaging
- 5mg
- Price
- $175
- Updated
- 2021/12/16
- Product number
- BISN0200
- Product name
- MK-8353
- Packaging
- 5mg
- Price
- $284
- Updated
- 2021/12/16
- Product number
- BISN0200
- Product name
- MK-8353
- Packaging
- 25mg
- Price
- $804
- Updated
- 2021/12/16
- Product number
- CS-0040548
- Product name
- MK-8353
- Purity
- 98.79%
- Packaging
- 50mg
- Price
- $1260
- Updated
- 2021/12/16
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
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