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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。
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 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 477 | 现货 | |
5 mg | ¥ 1,160 | 现货 | |
10 mg | ¥ 1,780 | 现货 | |
25 mg | ¥ 3,070 | 现货 | |
50 mg | ¥ 4,350 | 现货 | |
100 mg | ¥ 5,870 | 现货 | |
200 mg | ¥ 7,890 | 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 |
Smiles | NC1=C2C(=C(C=N1)C3=CN(CCO)N=C3)SC=C2C4=CC=C(NC(NC5=CC(F)=CC=C5)=O)C=C4 |
密度 | 1.47 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 55 mg/mL (112.58 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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