SCH900353
- MK 8353
- Optical Purity: 0.99
- Soluble in DMSO
- MF: C37H41N9O3S
- MW: 691.84
Description
SCH900353 is an orally bioavailable potent inhibitor targeting activated ERK1/2 with IC50 values of 23.0 and 8.8 nM, respectively, and nonactivated ERK2 with IC50 of 0.5 nM, highly selective over a panel of 227-human kinase; decreases levels of pERK1, pERK2, and ribosomal S6 kinase (pRSK) protein formation, with complete suppression of pERK1 and pERK2 observed at 30 nM in A2058 cells; inhibits the in vitro proliferation of a panel of BRAFV600-mutant and RAS-mutant cancer cell lines; displays in vivo antitumor efficacy against BRAFV600 mutant Colo-205 colon cancer model and the BRAFV600 mutant SK-MEL-28 melanoma model.
More Information
| Parent CAS No. | 1184173-73-6 |
|---|---|
| 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)-5,6-dihydropyridin-1(2H)-yl)-2-oxoethyl)-3-(methylthio)pyrrolidine-3-carboxamide |
| extra_info | Sold in collaboration with Chemietek |
| SMILES | C12NN=C(C3C=NC(OC(C)C)=CC=3)C=1C=C(NC(=O)[C@@]1(SC)CN(CC(N3CCC(C4C=CC(C5=NN(C)C=N5)=CC=4)=CC3)=O)CC1)C=C2 |&1:20,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C37H41N9O3S/c1-24(2)49-32-12-9-28(20-38-32)34-30-19-29(10-11-31(30)41-42-34)40-36(48)37(50-4)15-18-45(22-37)21-33(47)46-16-13-26(14-17-46)25-5-7-27(8-6-25)35-39-23-44(3)43-35/h5-13,19-20,23-24H,14-18,21-22H2,1-4H3,(H,40,48)(H,41,42)/t37-/m0/s1 |
| InChiKey | KPQQGHGDBBJGFA-QNGWXLTQSA-N |
| CID | 58282870 |
| Short Description | ERK1/2 inhibitor |
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