(Z)-Orantinib ((Z)-SU6668) 是一种有效,选择性,具有口服活性和 ATP 竞争性的Flk‐1/KDR,PDGFRβ和FGFR1抑制剂,IC50值分别为 2.1,0.008 和 1.2 μM。(Z)-Orantinib 是有效的抗血管生成和抗肿瘤剂,可诱导已建立的肿瘤消退。
生物活性 | (Z)-Orantinib ((Z)-SU6668) is a potent, selective, orally active and ATP competitive inhibitor ofFlk‐1/KDR,PDGFRβ, andFGFR1, withIC50s of 2.1, 0.008, and 1.2 μM, respectively. (Z)-Orantinib is a potent antiangiogenic and antitumor agent that induces regression of established tumors[1][2]. |
IC50& Target[2] | Flk-1/KDR 2.1 μM (IC50) | PDGFRβ 0.008 μM (IC50) | FGFR1 1.2 μM (IC50) |
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体外研究 (In Vitro) | SU6668 (5-15 min) inhibits Flk-1 trans-phosphorylation (Ki=2.1 μM), FGFR1 trans-phosphorylation (Ki=1.2 μM), and PDGFR autophosphorylation (Ki=0.008 μM)[1]. SU6668 (0.03-10 μM; 60 min) inhibits the VEGF-stimulated increase of KDR tyrosine phosphorylation in HUVECs[1]. SU6668 inhibits mitogenesis of HUVECs induced by both VEGF and FGF in a dose-dependent manner with IC50s of 0.34 and 9.6 μM, respectively[1].
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体内研究 (In Vivo) | SU6668 (4-200 mg/kg/day; p.o. for 21 d) induces dose-dependent inhibition of A431 tumor growth in athymic mice[1]. SU6668 (75 mg/kg/day; i.p. for 22 d) significantly suppresses tumor angiogenesis and vascularization in mice[1]. SU6668 (200 mg/kg/day; p.o. for 11-27 d) induces striking regression of large established A431 xenografts in athymic mice[1].
Animal Model: | Female athymic mice (BALB/c,nu/nu) were implanted A431 tumor cells[1] | Dosage: | 4, 40, 75, 200 mg/kg | Administration: | P.o. daily for 21 days | Result: | Induced 97% growth inhibition against A431 tumor at the dose of 97%. No mortality was observed in any treatment group. |
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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 : 50 mg/mL(161.11 mM;Need ultrasonic) 配制储备液 1 mM | 3.2222 mL | 16.1108 mL | 32.2217 mL | 5 mM | 0.6444 mL | 3.2222 mL | 6.4443 mL | 10 mM | 0.3222 mL | 1.6111 mL | 3.2222 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 (6.70 mM); Suspended solution; Need ultrasonic
此方案可获得 2.08 mg/mL (6.70 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 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 (6.70 mM); Suspended solution; Need ultrasonic
此方案可获得 2.08 mg/mL (6.70 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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