Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ilorasertib (ABT-348) 是一种 ATP 竞争性多靶点激酶抑制剂,可抑制 Aurora A、Aurora B 和Aurora C,IC50值为120 nM、7 nM 和1 nM。它还抑制 RET 酪氨酸激酶、PDGFRβ 和 Flt1,IC50为7 nM、3 nM 和 32 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 987 | 现货 | ||
2 mg | ¥ 1,520 | 现货 | ||
5 mg | ¥ 2,170 | 现货 | ||
10 mg | ¥ 2,970 | 现货 | ||
25 mg | ¥ 5,120 | 现货 | ||
50 mg | ¥ 7,260 | 现货 | ||
100 mg | ¥ 9,790 | 现货 | ||
500 mg | ¥ 19,600 | 现货 |
产品描述 | Ilorasertib (ABT-348) (ABT-348) is an ATP-competitive multitargeted kinase inhibitor, which inhibits Aurora A/Aurora B/Aurora C (IC50s: 120 nM/7 nM/1 nM). It also suppresses RET tyrosine kinase, PDGFRβ, and Flt1 (IC50s: 7 nM, 3 nM, and 32 nM). |
靶点活性 | FLT3:1 nM, Aurora A:120 nM, PDGFRβ:13 nM, Aurora B:7 nM, PDGFRα:11 nM, Aurora C:1 nM, VEGFR1:1 nM, VEGFR2:2 nM |
体外活性 | 除了针对Aurora激酶外,Ilorasertib还是VEGFR和PDGFR激酶家族的强效抑制剂,并在较小程度上抑制Src家族的胞质酪氨酸激酶。Ilorasertib能够依赖浓度地增加两种NSCLC细胞系展现多倍体的程度和数量(EC50: 5, 10 nM)。Ilorasertib对表达BCR-ABL的CML细胞以及表达Gleevec抗性BCR-ABL T315I突变的细胞显示出抗增殖活性(IC50: 47, 260 nM)[2]。 |
体内活性 | Ilorasertib 在子宫水肿模型中有效抑制 VEGF 反应(ED50:0.2 mg/kg,静脉注射)。 Ilorasertib (25 mg/kg, s.c.) 可抑制从移植白血病模型获得的循环肿瘤细胞中的组蛋白 H3 磷酸化。 Ilorasertib(20 mg/kg,口服)可抑制人类异种移植模型中已形成肿瘤的生长并导致晚期肿瘤消退[2]。 Ilorasertib 在实体和血液异种移植模型中每周一次静脉、微型泵或肠胃外给药后显示出显着的抗肿瘤功效[3]。 |
细胞实验 | Noncycling primary HUVEC are used to assess the effect of Ilorasertib on nonproliferating cells. Cells (35,000/well) are seeded in growth medium in a 96-well tissue culture plate, and after 2 days, the medium is changed and the cells are treated with Ilorasertib. After an additional 3 days, cell viability is measured with Cell TiterGlo reagent [2]. |
动物实验 | For flank xenograft models, cells are suspended in PBS, mixed with Matrigel (phenol red-free) in a ratio of 1:4 (v/v), and inoculated into the flank of female SCID/beige mice (5 million cells per site). Inoculated mice are randomized into groups of 10, and treatment is initiated when mean tumor volume is approximately 0.4 cm^3 or 0.5 cm^3. Tumor growth in the flank is assessed by measuring tumor size with calipers and calculating volume using the formula (L × W2/2). Study groups are terminated before tumor volume reaches 3 cm^3. Inhibition of tumor growth is assessed at the time the vehicle-treated group is terminated by calculating the ratio of the mean volume of the test drug group to the mean volume of the untreated (control) group (T/C) and calculating the percentage of inhibition of control [(1 ? T/C) × 100]. The dosing formulation of test agents is prepared by stepwise addition, with mixing, of the following reagents: EtOH, Tween 80, polyethylene glycol 400, and 2% hydroxypropyl methylcellulose (2:5:20:73, v/v). The dosing volume is 10 mL/kg [2]. |
别名 | ABT-348 |
分子量 | 488.54 |
分子式 | C25H21FN6O2S |
CAS No. | 1227939-82-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 40 mg/mL (81.87 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.0469 mL | 10.2346 mL | 20.4692 mL | 51.1729 mL |
5 mM | 0.4094 mL | 2.0469 mL | 4.0938 mL | 10.2346 mL | |
10 mM | 0.2047 mL | 1.0235 mL | 2.0469 mL | 5.1173 mL | |
20 mM | 0.1023 mL | 0.5117 mL | 1.0235 mL | 2.5586 mL | |
50 mM | 0.0409 mL | 0.2047 mL | 0.4094 mL | 1.0235 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。
Ilorasertib 1227939-82-3 Angiogenesis Apoptosis Cell Cycle/Checkpoint Chromatin/Epigenetic Tyrosine Kinase/Adaptors VEGFR FLT c-RET PDGFR Aurora Kinase anti-tumor H1299 ABT348 Platelet-derived growth factor receptor Inhibitor antiproliferative activity AML histone H3 phosphorylation ABT-348 Vascular endothelial growth factor receptor inhibit H460 cells MDS ABT 348 inhibitor