Chiauranib (CS2164) 是一种针对肿瘤血管生成的具有口服活性的多靶点抑制剂。Chiauranib 有效抑制血管生成相关激酶 (VEGFR1，VEGFR2，VEGFR3，PDGFRα和c-Kit)，有丝分裂相关激酶Aurora B和慢性炎症相关激酶CSF-1R，IC50值为 1-9 nM。Chiauranib 具有很强的抗癌作用。
| 生物活性 | Chiauranib (CS2164) is an orally active multi-target inhibitor against tumor angiogenesis. Chiauranib potently inhibits the angiogenesis-related kinases (VEGFR1,VEGFR2,VEGFR3,PDGFRαandc-Kit), mitosis-related kinaseAurora B, and chronic inflammation-related kinaseCSF-1R, withIC50values ranging from 1-9 nM. Chiauranib has strongly anticancer effects[1]. |
| IC50& Target[1] | Flt-1 8 nM (IC50) | KDR 7 nM (IC50) | Flt-4 9 nM (IC50) | PDGFRα 1 nM (IC50) | Aurora B 9 nM (IC50) | PDGFRβ 93 nM (IC50) | c-Kit 4 nM (IC50) | CSF-1R 7 nM (IC50) |
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体外研究
(In Vitro) | Chiauranib (CS2164; 3 μM; 24 hours) shows induction of G2/M cell cycle arrest and suppression of cell proliferation in tumor tissues through the inhibition of Aurora B-mediated H3 phosphorylation[1].
In HUVEC and PDGFRβ phosphorylation in PDGFRβ overexpressed NIH3T3 cells, Chiauranib (CS2164; 0.03-3 μM) displays anti-angiogenic activities through suppression of VEGFR/PDGFR phosphorylation, inhibition of ligand-dependent cell proliferation and capillary tube formation, and prevention of vasculature formation in tumor tissues[1].
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Chiauranib (CS2164) inhibits CSF-1R phosphorylation that leads to the suppression of ligand-stimulated monocyte-to-macrophage differentiation and reduces CSF-1R+cells in tumor tissues[1].
Cell Cycle Analysis[1] | Cell Line: | Molt-4 cells | | Concentration: | 3 μM | | Incubation Time: | 24 hours | | Result: | Induced the pronounced cell cycle arrest in the G2/M phase at 3 μM. |
Western Blot Analysis[1] | Cell Line: | Molt-4 cells | | Concentration: | 1.5 μM, 3 μM, 6 μM | | Incubation Time: | 24 hours | | Result: | Yielded a substantial reduction in the level of p-H3 in Molt‐4 cells in a concentration-dependent fashion. |
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体内研究
(In Vivo) | Chiauranib (CS2164; 0.5-40 mg/kg; oral administration; once daily; for 33 days or 43 days) treatment induces remarkable regression or complete inhibition of tumor growth at well-tolerated oral doses in several human tumor xenograft models. Chiauranib exhibits broad and potent in vivo anti-tumor activities[1].
| Animal Model: | Female BALB/c athymic (nu+/nu+) mice (6-week old) bearing HCT-8, SMMC-7721, MGC‐803 or A549 cells[1] | | Dosage: | 2.5 mg/kg, 5 mg/kg, 10 mg/kg, 20 mg/kg, 40 mg/kg | | Administration: | Oral administration; once daily; for 33 days or 43 days | | Result: | Induced remarkable regression or complete inhibition of tumor growth in several human tumor xenograft models. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
| 溶解性数据 | In Vitro: DMSO : 62.5 mg/mL(143.52 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.2964 mL | 11.4818 mL | 22.9637 mL | | 5 mM | 0.4593 mL | 2.2964 mL | 4.5927 mL | | 10 mM | 0.2296 mL | 1.1482 mL | 2.2964 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 (protect from light)。-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 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (4.78 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.78 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 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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