| 生物活性 | Ilorasertib (ABT-348) is a potent, orally active and ATP-competitiveaurorainhibitor withIC50s of116, 5, 1 nM foraurora A,aurora B,aurora C, respectively. Ilorasertib also is a potentVEGF,PDGFinhibitor. Ilorasertib has the potential for the research of acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS)[1][2]. |
| IC50& Target[1] | Aurora C 1 nM (IC50) | Aurora B 7 nM (IC50) | Aurora B (Y156H) 12 nM (IC50) | Aurora A 120 nM (IC50) | PDGFRα 11 nM (IC50) | PDGFRβ 13 nM (IC50) | VEGFR1 1 nM (IC50) | VEGFR2 2 nM (IC50) | VEGFR3 43 nM (IC50) | FLT3 1 nM (IC50) | CSF-1R 3 nM (IC50) | c-KIT 20 nM (IC50) |
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体外研究
(In Vitro) | Ilorasertib (0, 3, 10, 30 nM; 24 h) induces a concentration-dependent increase in the extent and number of H1299, H460 cells[2].
Ilorasertib (1-1000 nM) shows antiproliferative activity[2].
Cell Viability Assay[2] | Cell Line: | H1299, H460 cells | | Concentration: | 0, 3, 10, 30 nM | | Incubation Time: | 24 h | | Result: | Induced a concentration-dependent increase in the extent and number of cells exhibiting polyploidy with EC50S of 5, 10 nM for H1299, H460 cells, respectively. |
Cell Proliferation Assay[2] | Cell Line: | MV-4-11, SEM, K562, HCT-15, SW620, H1299, H460 cells | | Concentration: | 1-1000 nM | | Incubation Time: | | | Result: | Showed antiproliferative activity with IC50s of 0.3, 1, 103, 6, 6, 2, 2 nM for MV-4-11, SEM, K562, HCT-15, SW620, H1299, H460 cells, respectively. |
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体内研究
(In Vivo) | Ilorasertib (6.25, 12.5, 25 mg/kg; p.o.) shows anti-tumor activity in MV-4-11 tumor-bearing SCID mice with TGI of 80%, 86%, 94% at 6.25, 12.5, 25 mg/kg, respectively[1].
Ilorasertib (6.25, 12.5, 25 mg/kg; p.o.) shows anti-tumor activity in SKM-1 tumor-bearing SCID mice with TGI of 38%, 59%, 80% at 6.25, 12.5, 25 mg/kg, respectively[1].
Ilorasertib (0, 3.75, 7.5, 15 mg/kg; i.p.) inhibits the histone H3 phosphorylation at 4-8 h in blood-borne tumor cells[2].
Ilorasertib (0.2 mg/kg; i.v.) shows anti-VEGF activity in mouse[2].
Ilorasertib (20 mg/kg; p.o.;once weekly for 3 weeks) shows anti-tumor activity in mouse[2].
| Animal Model: | Female SCID/beige mice[2] | | Dosage: | 25 mg/kg | | Administration: | Subcutaneous minipump; 24 h | | Result: | Inhibited the histone H3 phosphorylation and the tumor drug concentration associated with 50% inhibition of histone H3 phosphorylation. |
| Animal Model: | 22-26 g, female NOD/SCID mice (xenograft model of multiple myeloma (KMS11))[2] | | Dosage: | 20 mg/kg | | Administration: | P.o.; once weekly for 3 weeks | | Result: | Inhibited the tumor growth in mouse. |
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| Clinical Trial | |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 41.67 mg/mL(85.29 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.0469 mL | 10.2346 mL | 20.4692 mL | | 5 mM | 0.4094 mL | 2.0469 mL | 4.0938 mL | | 10 mM | 0.2047 mL | 1.0235 mL | 2.0469 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (4.26 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.26 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: 2.08 mg/mL (4.26 mM); Suspended solution; Need ultrasonic
此方案可获得 2.08 mg/mL (4.26 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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