H3B-5942
Cat. No.：YN480544
CAS No. ：2052128-15-9
规格
价格(RMB)
库存
| 产品名称: | H3B-5942 |
| CAS No.: | 2052128-15-9 |
| Chemical Name: | (2E)-4-[[2-[4-[(1E)-1-(1H-indazol-5-yl)-2-phenyl-1-buten-1-yl]phenoxy]ethyl]amino]-N,N-dimethyl-2-butenamide |
| Synonyms: | H3B5942 |
| 分子量: | 494.63 |
| 分子式: | C₃₁H₃₄N₄O₂ |
| SMILES: | CC/C(C1=CC=CC=C1)=C(C2=CC=C(OCCNC/C=C/C(N(C)C)=O)C=C2)\C3=CC(C=NN4)=C4C=C3 |
| 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: | H3B-5942 是一种选择性、不可逆、可口服的estrogen receptor共价拮抗剂，能够靶作用于 Cys530，使野生型和突变型ERα失活，Ki值分别为 1 nM 和 0.41 nM。H3B-5942 能够减少 ERα 的目标基因GREB1的表达。H3B-5942 具有抗癌作用，对含有 ERαWT或者突变型 ERα 的肿瘤细胞和动物具有抗肿瘤活性。 |
| IC50和靶点: | [{name:"ERαY537S:0.41 nM (Ki)"},{name: "ERαWT:1 nM (Ki)"}] |
| In Vitro: | |
| In Vivo: | |
| Clinical Trial: | |
| Solvent & Solubility: |
Puyang, X., Furman, C., Zheng, G.Z., et al.Discovery of selective estrogen receptor covalent antagonists for the treatment of ERαWT and ERαMUT breast cancerCancer Discov.8(9),1176-1193(2018)
