化合物Prexasertib T4310

Product Introduction
Bioactivity


英文名: Prexasertib

描述: Prexasertib (LY2606368) 是一种具有潜在抗肿瘤活性的检查点激酶 1 抑制剂。它可引起双链 DNA 断裂和复制突变，导致细胞凋亡。

细胞实验: LY2606368 is broadly antiproliferative with IC50s of 3 nM, 3 nM, 10 nM, 37 nM, and 68 nM against U-2 OS, Calu-6, HT-29, HeLa, and NCI-H460 cell lines, respectively. LY2606368 (25 μM) exhibits inhibitory activities against proliferation of AGS and MKN1 cells. LY2606368 (20 nM) inhibits HR repair capacity DR-GFP cells.

动物实验: LY2606368 is formulated in vehicle consisting of 20% Captisol.Female CD-1 nu-/nu- mice (26-28 g) are used for this study. Tumor growth is initiated by subcutaneous injection of 1×106 Calu-6 cells in a 1:1 mixture of serum-free growth medium and Matrigel in the rear flank of each subject animal. When tumor volumes reach approximately 150 mm3 in size, the animals are randomized by tumor size and body weight, and placed into their respective treatment groups. Vehicle consisting of 20% Captisol pH4 or LY2606368 is administered by subcutaneous injection in a volume of 200 μL. Four, eight, 12, 24, and 48 hours after drug administration, blood for plasma drug exposure is extracted via cardiac puncture and assayed on a Sciex API 4000 LC/MS-MS system. The xenograft tissue is promptly removed and prepared. Lysates are analyzed by immunoblot analysis for protein phosphorylation levels. Group means, SEs and P values are calculated using Kronos.

体外活性: LY2606368 potently abrogates the G2-M checkpoint activated by doxorubicin in p53-deficient HeLa cells(EC50=9 nM). LY2606368 is a potent and selective ATP competitive inhibitor of Chk1(IC50 <1 nM), and also inhibits CHK2(IC50=8 nM).

体内活性: In xenograft tumor models, LY2606368 (15 mg/kg, s.c.) significantly inhibits tumor growth with less animal weight loss.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : < 1 mg/mL (insoluble or slightly soluble)


关键字: SIK | Prexasertib | Checkpoint Kinase (Chk) | HT-29 | S296 | Apoptosis | DNA | double-stranded | inhibit | autophosphorylation | LY-2606368 | H2AX | ATP-competitive | HeLa | MELK | RSK1 | CDK2 | Inhibitor | S516 | ARK5 | replication | BRSK2 | CDC25A | LY 2606368

相关产品: Ziyuglycoside II | Tanespimycin | GGTI298 Trifluoroacetate | BI-6C9 | MK-2206 dihydrochloride | Anticancer agent 130 | DB1976 | Ruxolitinib | 7,8-Dihydroxyflavone | Pranoprofen

相关库: Drug Repurposing Compound Library | Anti-Breast Cancer Compound Library | Anti-Cancer Drug Library | Clinical Compound Library | Bioactive Compounds Library Max | Kinase Inhibitor Library | Inhibitor Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Active Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途