BAY-1125976
BAY-1125976 is a potent and selective allosteric AKT1/2 inhibitor. BAY-1125976 exhibits high efficacy on AKT signaling-dependent tumor growth in mouse models. BAY 1125976 potently and selectively inhibited the activity of full-length AKT1 and AKT2 by binding into an allosteric binding pocket formed by kinase and PH domain. In vitro, BAY 1125976 inhibited cell proliferation in a broad panel of human cancer cell lines. BAY 1125976 exhibited strong in vivo efficacy in both cell line and patient-derived xenograft models such as the KPL4 breast cancer model (PIK3CAH1074R mutant), the MCF7 and HBCx-2 breast cancer models and the AKTE17K mutant driven prostate cancer (LAPC-4) and anal cancer (AXF 984) models.
仅供研究使用。 我们不向患者出售。
化学信息
| 名称 | BAY-1125976 |
|---|---|
| Iupac 化学名称 | Imidazo[1,2-b]pyridazine-6-carboxamide, 2-[4-(1-aminocyclobutyl)phenyl]-3-phenyl- |
| 同义词 | BAY-1125976; BAY 1125976; BAY1125976; |
| 英文同义词 | BAY-1125976; BAY 1125976; BAY1125976; |
| 分子式 | C23H21N5O |
| 分子量 | 383.45 |
| Smile | O=C(C1=NN2C(C=C1)=NC(C3=CC=C(C4(N)CCC4)C=C3)=C2C5=CC=CC=C5)N |
| InChiKey | JBGYKRAZYDNCNV-UHFFFAOYSA-N |
| InChi | InChI=1S/C23H21N5O/c24-22(29)18-11-12-19-26-20(21(28(19)27-18)16-5-2-1-3-6-16)15-7-9-17(10-8-15)23(25)13-4-14-23/h1-3,5-12H,4,13-14,25H2,(H2,24,29) |
| Cas号 | 1402608-02-9 |
| 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 | 类白色固体 |
|---|---|
| 纯度 | 98% Min. |
| 存储 | 0-4℃，可保存几天到几周；-20℃，可保存 几个月。 |
| 可溶性 | 溶于DMSO等有机溶剂 |
| 处理方式 | |
| 运输条件 | 可以在室温下进行运输。 |
| 海关编码 |
| Targets | |
|---|---|
| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
1: Politz O, Siegel F, Bärfacker L, Bömer U, Hägebarth A, Scott WJ, Michels M,
Ince S, Neuhaus R, Meyer K, Fernández-Montalván AE, Liu N, von Nussbaum F,
Mumberg D, Ziegelbauer K. BAY 1125976, a selective allosteric AKT1/2 inhibitor,
exhibits high efficacy on AKT signaling-dependent tumor growth in mouse models.
Int J Cancer. 2017 Jan 15;140(2):449-459. doi: 10.1002/ijc.30457. Epub 2016 Oct
20. PubMed PMID: 27699769.
