SCH772984
Cat. No.:YN350211
产品名称: | SCH772984 |
CAS No.: | 942183-80-4 |
Chemical Name: | (3R)-1-[2-oxo-2-[4-[4-(2-pyrimidinyl)phenyl]-1-piperazinyl]ethyl]-N-[3-(4-pyridinyl)-1H-indazol-5-yl]-3-pyrrolidinecarboxamide |
Synonyms: | SCH 772984; SCH772984 |
分子量: | 587.67 |
分子式: | C₃₃H₃₃N₉O₂ |
SMILES: | O=C([C@H](CC1)CN1CC(N(CC2)CCN2C(C=C3)=CC=C3C4=NC=CC=N4)=O)NC5=CC6=C(C=C5)NN=C6C7=CC=NC=C7 |
存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
运输: | Room temperature in continental US; may vary elsewhere. |
产品描述: | SCH772984 是一种高选择性和 ATP 竞争性ERK抑制剂,对 ERK1 和 ERK2 的IC50分别为 4 和 1 nM。SCH772984 在对天然 MAPK 抑制和耐药 MAPK 抑制的细胞中的BRAF或RAS突变,具有抗肿瘤活性。 |
IC50和靶点: | [{name:"ERK2:1 nM (IC50)"},{name: "ERK1:4 nM (IC50)"}] |
In Vitro: | |
In Vivo: | |
Clinical Trial: | |
Solvent & Solubility: |
Seger, R., and Krebs, E.G.The MAPK signaling cascadeFASEB J.9,726-735(1995)
Morris, E.J., Jha, S., Restaino, C.R., et al.Discovery of a novel ERK inhibitor with activity in models of acquired resistance to BRAF and MEK inhibitorsCancer Discov.3(7),742-750(2013)
Cahikaud, A., Tacconi, E., Zimmer, J., et al.A unique inhibitor binding site in ERK1/2 is associated with slow binding kineticsNat. Chem. Biol.10(10),853-860(2014)