Quisinostat dihydrochloride (JNJ-26481585 dihydrochloride) 是一种有口服活性,高效的 pan-HDAC抑制剂,对 HDAC1,HDAC2,HDAC4,HDAC10,HDAC11 的IC50值分别为 0.11 nM,0.33 nM,0.64 nM,0.46 nM 和 0.37 nM。Quisinostat dihydrochloride 具有广泛的抗肿瘤活性。
生物活性 | Quisinostat dihydrochloride (JNJ-26481585 dihydrochloride) is an orally available, potent pan-HDACinhibitor withIC50s of 0.11 nM, 0.33 nM, 0.64 nM, 0.46 nM, and 0.37 nM forHDAC1,HDAC2,HDAC4,HDAC10andHDAC11, respectively. Quisinostat dihydrochloride has a broad spectrum antitumoral activity[1]. |
IC50& Target[1] | HDAC1 0.11 nM (IC50) | HDAC2 0.33 nM (IC50) | HDAC11 0.37 nM (IC50) | HDAC10 0.46 nM (IC50) | HDAC5 3.69 nM (IC50) | HDAC8 4.26 nM (IC50) | HDAC3 4.86 nM (IC50) | HDAC9 32.1 nM (IC50) | HDAC6 76.8 nM (IC50) | HDAC7 119 nM (IC50) |
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体外研究 (In Vitro) | JNJ-26481585 inhibits HDAC isozymes in vitro[1]. JNJ-26481585 (30-1000 nM; 24 hours) is a potent pan-HDAC inhibitor in tumor cells[1]. JNJ-26481585 has broad spectrum antiproliferative activity against solid and hematologic cancer cell lines and induces apoptosis[1].
Western Blot Analysis[1] Cell Line: | Human A2780 ovarian carcinoma cells | Concentration: | 30 nM, 100 nM, 300 nM, 1000 nM | Incubation Time: | 24 hours | Result: | Induced H3 and H4 acetylation at concentrations as low as 30 to 100 nM. |
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体内研究 (In Vivo) | JNJ-26481585 (40 mg/kg; p.o.; once daily, for 3 days) as a potent HDAC1 inhibitor p21waf1,cip1 ZsGreen tumors in vivo[1]. JNJ-26481585 induces continuous H3 acetylation in tumor tissue in vivo[1]. JNJ-26481585 (10 mg/kg; once daily; i.p.; for 14 days) strongly inhibits the growth of large pre-established HCT116 colon xenografts[1].
Animal Model: | NMRI nude mice, with HCT116 colon carcinoma cells xenografts[1] | Dosage: | 10 mg/kg | Administration: | Intraperitoneal injection, once daily, for 14 days | Result: | Strongly inhibited the growth of large pre-established HCT116 colon xenografts. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
溶解性数据 | In Vitro: DMSO : 31.25 mg/mL(66.86 mM;ultrasonic and warming and heat to 70℃) 配制储备液 1 mM | 2.1395 mL | 10.6977 mL | 21.3954 mL | 5 mM | 0.4279 mL | 2.1395 mL | 4.2791 mL | 10 mM | 0.2140 mL | 1.0698 mL | 2.1395 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 (sealed storage, away from moisture)。-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 (4.45 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.45 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 (4.45 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.45 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。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (4.45 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.45 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 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 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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