理化性质和储存条件
| Molecular Weight (MW) | 691.84 |
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| Formula | C37H41N9O3S |
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| CAS No. | 1184173-73-6 (free base) |
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| Storage | -20℃ for 3 years in powder form |
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| -80℃ for 2 years in solvent |
| Solubility (In vitro) | DMSO: ≥ 50 mg/mL |
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| Water: < 1mg/mL |
| Ethanol: < 1mg/mL |
| Chemical Name | (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 |
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| Synonyms | MK-8353; SCH-900353; MK 8353; SCH900353; MK8353; SCH 900353 |
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| SMILES Code | O=C(CN1CC[C@@](SC)(C(NC2=CC=C(NN=C3C4=CC=C(OC(C)C)N=C4)C3=C2)=O)C1)N5CCC(C6=CC =C(C7=NN(C)C=N7)C=C6)=CC5 |
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实验参考方法
MK-8353 (also known as SCH900353; SCH-900353) is a novel, potent, selective and orally bioavailable ERK inhibitor with anticancer activity. It ERK1/2 with IC50 values of 23.0 nM and 8.8 nM, respectively, in an IMAP kinase assay and an IC50 of 0.5 nM for nonactivated ERK2 in a MEK1-ERK2-coupled assay. MK-8353 exhibited comparable potency with SCH772984 across various preclinical cancer models. Forty-eight patients were enrolled in the P07652 study, and twenty-six patients were enrolled in the MK-8353-001 study. Adverse events included diarrhea (44%), fatigue (40%), nausea (32%), and rash (28%). Dose-limiting toxicity was observed in the 400-mg and 800-mg dose cohorts. Sufficient exposure to MK-8353 was noted that correlated with biological activity in preclinical data. Three of fifteen patients evaluable for treatment response in the MK-8353-001 study had partial response, all with BRAFV600-mutant melanomas.
These protocols are for reference only. InvivoChem does not independently validate these methods.
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