Linsitinib产品描述：Linsitinib 是一种选择性的 IGF-1R 抑制剂，IC₅₀ 值为 35 nM，也适度地作用于 InsR，IC₅₀ 值为 75 nM；对 Abl，ALK，BTK，EGFR，FGFR1/2，PKA 等没有作用。
Linsitinib产品描述：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.IC50 & Target: IC50: 35 nM (IGF-1R), 75 nM (InsR)In Vitro: Linsitinib 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. Linsitinib enables an intermediate conformation of the target protein through interactions with the C-helix. Linsitinib displays favorable metabolic stability in liver microsomes. Linsitinib fully inhibits both IR ａnd IGF-1R phosphorylation at a concentration of 1 μM. Linsitinib inhibits proliferation of several tumor cell lines including non-small-cell lung cancer ａnd colorectal cancer (CRC) tumor cell line with EC₅₀ of 0.021 to 0.810 μM^[1]. In Vivo: Linsitinib 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. Linsitinib 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. Linsitinib 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 Linsitinib dose. Linsitinib elevates the blood glucose levels at a dose of 25 mg/kg after 12 days administration. Linsitinib 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^[1]. Linsitinib 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. Linsitinib inhibits the growth of tumors in NCI-H292 xenograft mouse model^[2].

研究领域：Protein Tyrosine Kinase/RTK

靶点：FLT3

相关产品：Sorafenib | Cabozantinib | Gilteritinib | Quizartinib | Pacritinib | LY2784544 | CHIR-124 | UNC2025 | AST 487 | SB1317 | TG101209 | DCC-2036 | KW-2449 | Amuvatinib | AMG 925 |

Alternative_Names:OSI-906

MWt:421.49

Formula:C26H23N5O

SMILES:O[C@@]1(C)C[C@@H](C2=NC(C3=CC=C4C=CC(C5=CC=CC=C5)=NC4=C3)=C6C(N)=NC=CN62)C1

Research_Area:Cancer



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