| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| G407793-1ml |
1ml |
现货  |
|
| 英文别名 | RG-7603 | Urea, N-ethyl-N'-[4-[5,6,7,8-tetrahydro-4-[(3S)-3-methyl-4-morpholinyl]-7-(3-oxetanyl)pyrido[3,4-d]pyrimidin-2-yl]phenyl]- |
|---|---|
| 规格或纯度 | 10mM in DMSO |
| 英文名称 | GDC-0349 |
| 生化机理 | GDC-0349 (RG-7603) 是一种强效、选择性 ATP 竞争性 mTOR 抑制剂，Ki值为 3.8 nM，对 PI3Kα 和其他 266 激酶的抑制作用为 790 倍。第一阶段 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | 丝氨酸/苏氨酸蛋白激酶 mTOR 抑制剂 |
| 产品介绍 |
GDC-0349 是一种有效的，ATP竞争性的选择性 mTOR 抑制剂，Ki 值为 3.8 nM。GDC-0349 抑制 mTORC1 和 mTORC2 复合体。 Information GDC-0349 GDC-0349 (RG-7603) is a potent and selective ATP-competitive inhibitor of mTOR with K i of 3.8 nM, 790-fold inhibitory effect against PI3Kα and other 266 kinases. Phase 1. GDC-0349 has remarkable selectivity over 266 kinases, including all isoforms of PI3K. GDC-0349 inhibits downstream markers of mTOR, including phospho-4EBP1 and phospho-Akt(S473) in an in vivo PK/PD study in mouse, consistent with an inhibition of both mTORC1 and mTORC2 complexes. In vivo GDC-0349 demonstrates pathway modulation and dose-dependent efficacy in mouse xenograft cancer models. When dosed orally once daily in athymic mice in a MCF7-neo/Her2 tumor xenograft model (PI3K mutation), GDC-0349 inhibits tumor growth in a dose-dependent manner. It is also efficacious in other xenograft models, including PC3 (PTEN ) and 786-O (VHL mutant). cell lines： Concentrations： Incubation Time： Powder Purity:≥99% |
| ALogP | 1.982 |
|---|---|
| hba_count | 5 |
| HBD Count | 2 |
| Rotatable Bond | 5 |
| 分子类型 | 小分子 |
|---|---|
| Canonical SMILES | CCNC(=O)NC1=CC=C(C=C1)C2=NC(=C3CCN(CC3=N2)C4COC4)N5CCOCC5C |
| 分子量 | 452.55 |
| Reaxy-Rn | 52178663 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=52178663&ln= |
| DMSO(mg / mL) Max Solubility | 91 |
|---|---|
| DMSO(mM) Max Solubility | 201.08 |
| Water(mg / mL) Max Solubility | <1 |
| Reaxy-Rn | 52178663 |
|---|---|
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=52178663&ln= |
| Concentration(Compounding value) | 9-11(mmol/L) |
|---|---|
| Appearance(G407793) | Light-yellow Liquid |
| Record the entire process by video | Conform |
首页
400-620-6333
