Migoprotafib
Migoprotafib, also known as GDC-1971 and RLY-1971, is a SHP2 allosteric inhibitor. GDC-1971 showed outstanding potency in biochemical and cell models, and it had a predicted human PK profile that suggested it would achieve target engagement at reasonable doses. GDC-1971 showed an IC50 below the limit of detection of the assay (≪0.001 μM), while that IC50 shifted to 0.17 μM in the same biochemical assay with the constitutively active E76K SHP2 mutant.
仅供研究使用。 我们不向患者出售。
化学信息
| 名称 | Migoprotafib |
|---|---|
| Iupac 化学名称 | (3R)-1'-[3-(3,4-dihydro-1,5-naphthyridin-1(2H)-yl)-1Hpyrazolo[3,4-b]pyrazin-6-yl]-spiro[benzofuran-2(3H),4'-piperidin]-3-amine |
| 同义词 | Migoprotafib; RLY-1971; RLY 1971; RLY1971; GDC-1971; GDC 1971; GDC1971; |
| 英文同义词 | Migoprotafib; RLY-1971; RLY 1971; RLY1971; GDC-1971; GDC 1971; GDC1971; |
| 分子式 | C25H26N8O |
| 分子量 | 454.53 |
| Smile | N[C@H]1C2(CCN(C3=CN=C4C(NN=C4N5CCCC6=NC=CC=C56)=N3)CC2)OC7=CC=CC=C17 |
| InChiKey | RGCGBFIARQENML-JOCHJYFZSA-N |
| InChi | InChI=1S/C25H26N8O/c26-22-16-5-1-2-8-19(16)34-25(22)9-13-32(14-10-25)20-15-28-21-23(29-20)30-31-24(21)33-12-4-6-17-18(33)7-3-11-27-17/h1-3,5,7-8,11,15,22H,4,6,9-10,12-14,26H2,(H,29,30,31)/t22-/m1/s1 |
| Cas号 | 2377352-49-1 |
| 相关CAS号 |
订购信息
| 包装 | 价格 | 库存 | 纯度 | 备货期 |
|---|---|---|---|---|
| 大货 | 询价 | 询价 | 询价 |
| 外观性状 | 固体粉末 |
|---|---|
| 纯度 | 98% Min. |
| 存储 | 短期（几天到几周）为0-4摄氏度，长期（几个月）为-20摄氏度 |
| 可溶性 | 溶于DMSO |
| 处理方式 | |
| 运输条件 | 作为非危险化学品在环境温度下装运。这种产品在正常运输和海关工作期间可以稳定几周. |
| 海关编码 |
| Targets | |
|---|---|
| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
Taylor AM, Williams BR, Giordanetto F, Kelley EH, Lescarbeau A, Shortsleeves K, Tang Y, Walters WP, Arrazate A, Bowman C, Brophy E, Chan EW, Deshmukh G, Greisman JB, Hunsaker TL, Kipp DR, Saenz Lopez-Larrocha P, Maddalo D, Martin IJ, Maragakis P, Merchant M, Murcko M, Nisonoff H, Nguyen V, Nguyen V, Orozco O, Owen C, Pierce L, Schmidt M, Shaw DE, Smith S, Therrien E, Tran JC, Watters J, Waters NJ, Wilbur J, Willmore L. Identification of GDC-1971 (RLY-1971), a SHP2 Inhibitor Designed for the Treatment of Solid Tumors. J Med Chem. 2023 Sep 29. doi: 10.1021/acs.jmedchem.3c00483. Epub ahead of print. PMID: 37774359.
