Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Rabusertib (IC-83) 是一种有效的选择性的Chk1抑制剂,IC50为 7 nM。它有潜在的化学增强活性,用于各种癌症和肿瘤治疗的试验。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 278 | 现货 | ||
2 mg | ¥ 393 | 现货 | ||
5 mg | ¥ 659 | 现货 | ||
10 mg | ¥ 995 | 现货 | ||
25 mg | ¥ 1,930 | 现货 | ||
50 mg | ¥ 3,180 | 现货 | ||
100 mg | ¥ 4,330 | 现货 | ||
200 mg | ¥ 6,170 | 现货 | ||
500 mg | ¥ 9,350 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 795 | 现货 |
产品描述 | Rabusertib (IC-83) is an inhibitor of the cell cycle checkpoint kinase 1 (chk1) with potential chemopotentiating activity. Rabusertib has been used in trials studying the treatment of Cancer, Solid Tumors, Advanced Cancer, Pancreatic Neoplasms, and Non-Small Cell Lung Cancer. |
靶点活性 | Chk1:7 nM |
体外活性 | Chk1 is an ATP-dependent serine-threonine kinase and a key component in the DNA replication-monitoring checkpoint system activated by double-stranded breaks (DSBs). Chk1 contributes to all currently defined cell cycle checkpoints, including G1/S, intra-S-phase, G2/M, and the mitotic spindle checkpoint. By inhibiting the activity of chk1, LY2603618 prevents the repair of DNA caused by DNA-damaging agents, thus potentiating the antitumor efficacies of various chemotherapeutic agents. However, preClinicalal data involving LY2603618 has not been published until now. [1] Inhibition of Chk1 is predicted to enhance the effects of antimetabolites, such as gemcitabine. [2] LY2603618 treatment impairs DNA synthesis, increases DNA damage (via mitotic defects), induces apoptosis, and has synergistic activity with pemetrexed, especially in p53 mutant tumor cells. [3] |
体内活性 | In xenograft models, LY2603618 delays tumor growth when given in combination with pemetrexed. [3] |
激酶实验 | Protein kinase assays are performed variously. Assays are performed on the following protein kinases: ABL, AKT1, ARG, CAMK2, CDK1, CDK2, CHK1, CHK2, DAPK1, EGFR, EPHA1, EPHB2, EPHB3, EPHB4, ERK1, ERK2, FES, FGFR1, FGFR3, FGFR4, FGR, HCK, HER2, INSR, JNK1, JNK2, LCK, MET, NTRK1, NTRK2, p38α, p38β, p38δ, p38γ, p70S6K, PDGFRα, PDGFRβ, PDK1, PKCα, ROCK2, ROS, RSK2, SGK1, SRC, SYK, TAK1, TYRO3, VEGFR2, VEGFR3, YES, ZAP70[1]. |
细胞实验 | LY2603618 is prepared in DMSO (10 mM) and stock, and then diluted 1000-fold into medium[1]. Cells are plated at 2.5×103 per well, on 96-well tissue culture plates and incubated for one cell doubling (18-24 h). Gemcitabine dilutions are set up by half-log steps across a final concentration range of 1-1000 nM. LY2603618 is prepared by dilutions in DMSO to 5000× final concentration, and then diluted 1000-fold into medium to generate 5× stocks for addition to wells. Approximately 24 h after Gemcitabine addition, LY2603618 is added. Each combination is done in triplicate. After a period of two cell doublings following LY2603618 addition, MTS/PMS reagent is added to each well according to the manufacturer's instructions. Absorbance is read on a Spectra Max 250 spectrophotometer at 490 nm and the data analyzed with GraphPad Prism 4.0. Dose-response curves are fit by non-linear regression, with bottom fits constrained to 0 % inhibition[1]. |
别名 | LY2603618, IC-83 |
分子量 | 436.3 |
分子式 | C18H22BrN5O3 |
CAS No. | 911222-45-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 11 mg/mL (25.2 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.292 mL | 11.46 mL | 22.92 mL | 57.3 mL |
5 mM | 0.4584 mL | 2.292 mL | 4.584 mL | 11.46 mL | |
10 mM | 0.2292 mL | 1.146 mL | 2.292 mL | 5.73 mL | |
20 mM | 0.1146 mL | 0.573 mL | 1.146 mL | 2.865 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Rabusertib 911222-45-2 Autophagy Cell Cycle/Checkpoint PI3K/Akt/mTOR signaling Chk PDK inhibit LY2603618 Inhibitor IC-83 IC 83 Checkpoint Kinase (Chk) LY 2603618 IC83 LY-2603618 inhibitor