| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| L408746-1ml |
1ml |
现货  |
|
| 别名 | 林西替尼 (OSI-906) |
|---|---|
| 英文别名 | (1s,3s)-3-(8-amino-1-(2-phenylquinolin-7-yl)imidazo[1,5-a]pyrazin-3-yl)-1-methylcyclobutanol |
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Linsitinib (OSI-906) |
| 生化机理 | Linsitinib (OSI-906) 是 IGF-1R 的选择性抑制剂，在无细胞实验中的 IC50 为 35 nM；对 InsR 有一定效力，IC50 为 75 nM，对 Abl、ALK、BTK、EGFR、FGFR1/2、PKA 等无活性。第 3 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 | 胰岛素样生长因子 I 受体抑制剂 胰岛素受体抑制剂 胰岛素受体相关受体抑制剂 |
| 产品介绍 |
Linsitinib is a potent, selective insulin-like growth factor-1 receptor (IGF-1R, IC50 = 35 nM) and insulin receptor (IR, IC50 = 75 nM) kinase inhibitor which works to block the autophosphorylation of IGF-1R and IR. Additionally, in vitro studies of Linsitinib have demonstrated its ability to inhibit the proliferation of multiple tumor cell lines.Linsitinib is a selective inhibitor of IGF-1R with IC50 of 35 nM, and modestly potent to InsR with IC50 of 75 nM, and has no activity towards Abl, ALK, BTK, EGFR, FGFR1/2, PKA etc. Information Linsitinib (OSI-906) Linsitinib (OSI-906) is a selective inhibitor of IGF-1R with IC50 of 35 nM in cell-free assays; modestly potent to InsR with IC50 of 75 nM, and no activity towards Abl, ALK, BTK, EGFR, FGFR1/2, PKA etc. Phase 3. OSI-906 inhibits IGF-1R autophosphorylation and activation of the downstream signaling proteins Akt, ERK1/2 and S6 kinase with IC50 of 0.028 to 0.13 μM. OSI-906 enables an intermediate conformation of the target protein through interactions with the C-helix. OSI-906 displays favorable metabolic stability in liver microsomes. OSI-906 fully inhibits both IR and IGF-1R phosphorylation at a concentration of 1 μM. OSI-906 inhibits proliferation of several tumor cell lines including non-small-cell lung cancer and colorectal cancer (CRC) tumor cell line with EC50\xa0of 0.021 to 0.810 μM. In vivo OSI-906 inhibits tumor growth in an IGF-1R-driven xenograft mouse model, with 100% TGI and 55% regression at a dose of 75 mg/kg and 60% TGI and no regression at a dose of 25 mg/kg.\xa0OSI-906 administration induces different elimination half-lives of itself in dog, rat and mice, the elimination half-lives are 1.18 hours, 2.64 hours and 2.14 hours, respectively. OSI-906 administration at different single dose once-daily in femal Sprague-Dawley rat and femal CD-1 mouse reveal that the Vmax is not dose-proportional to OSI-906 dose. OSI-906 elevates the blood glucose levels at a dose of 25 mg/kg after 12 days administration. OSI-906 administration at a single dose of 75 mg/kg in IGF-1R-driven full-length human IGF-1R (LISN) xenograft mouse model achieve maximal inhibition of IGF-1R phosphorylation (80%) between 4 and 24 hours with plasma drug concentrations of 26.6-4.77 μM. OSI-906 administered as a single dose of at 60 mg/kg in NCI-H292 xenografts mice inhibits uptake of glucose at 2, 4, and 24 hours post-treatment in vivo. OSI-906 inhibits the growth of tumors in NCI-H292 xenograft mouse model. cell lines：HL-60 and KG1a Concentrations：0.02-0.8 μM Incubation Time：3 days Powder Purity:≥99% |
| 分子类型 | 小分子 |
|---|---|
| Isomeric SMILES | CC1(CC(C1)C2=NC(=C3N2C=CN=C3N)C4=CC5=C(C=C4)C=CC(=N5)C6=CC=CC=C6)O |
| 分子量 | 421.51 |
| Reaxy-Rn | 25747541 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=25747541&ln= |
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