Prexasertib
作者：齐岳
发布时间：2023-09-13
16:57:59
点击数：
产品名称：Prexasertib
产品描述：
| 产品描述 | Prexasertib is an inhibitor of checkpoint kinase 1 (chk1) with potential antineoplastic activity. |
| 靶点活性 | Chk2:8 nM, Chk1:<1 nM |
| 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. |
| 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. |
| 别名 | LY2606368, 5-[[5-[2-(3-氨基丙氧基)-6-甲氧基苯基]-1H-吡唑-3-基]氨基]-2-吡嗪甲腈 |
| 分子量 | 365.4 |
| 分子式 | C18H19N7O2 |
| CAS No. | 1234015-52-1 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: <1mg/mL
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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