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MK-8353(SCH900353)

  Cat. No.:  DC20197   Featured
Chemical Structure
1184173-73-6
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Field of application
MK-8353 (SCH900353) is an orally bioavailable, selective, and potent ERK inhibitor that inhibits activated ERK1 and ERK2 in vitro, with IC50 values of 23.0 nM and 8.8 nM, respectively (IMAP kinase assay), and nonactivated ERK2, with an IC50 of 0.5 nM (MEK
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1184173-73-6
Chemical Name: MK-8353
Synonyms: (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)-N-(3-{6-[(propan-2-yl)oxy]pyridin-3-yl}-1H-indazol-5-yl)pyrrolidine-3-carboxamide;GTPL9974;BCP23615;MK8353;SCH900353;SCH 900353;A16838;(3S)-3-methylsulfanyl-1-[2-[4-[4-(1-methyl-1,2,4-triazol-3-yl)phenyl]-3,6-dihydro-2H-pyridin-1-yl]-2-oxoethyl]-N-[3-(6-propan-2-yloxypyridin-3-yl)-1H-indazol-5-yl]pyrrolidine-3-carboxamide;MK-8353;BDB
SMILES: S(C([H])([H])[H])[C@]1(C(N([H])C2C([H])=C([H])C3=C(C(C4=C([H])N=C(C([H])=C4[H])OC([H])(C([H])([H])[H])C([H])([H])[H])=NN3[H])C=2[H])=O)C([H])([H])N(C([H])([H])C(N2C([H])([H])C([H])=C(C3C([H])=C([H])C(C4N=C([H])N(C([H])([H])[H])N=4)=C([H])C=3[H])C([H])([H])C2([H])[H])=O)C([H])([H])C1([H])[H]
Formula: C37H41N9O3S
M.Wt: 691.8449
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: MK-8353 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.
Target: ERK2:8.8 nM (IC50) ERK1:23 nM (IC50)
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].
In Vitro: MK-8353 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. MK-8353 only at 1 μM shows >50% inhibition on 3 kinases (CLK2, FLT4, and Aurora B), and no other kinases tested are inhibited by >35% at 0.1 μM. MK-8353 also shows potent antitumor activity against various cancer cell lines, such Malme-3M cells (Melanoma), Colo-205 cells (Colon), NCI-H292 cells (Lung), A-549 cells (NSCLC), 8505C cells (Thyroid), SW-626 cells (Ovarian), with EC50s of 21 nM, 19 nM, 130 nM, 230 nM, 210 nM, 108 nM[1].
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
MSDS
COA
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2018-0101
2018-0101
2018-0101
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