Quisinostat dihydrochloride JNJ-26481585 dihydrochloride|cas:875320-31-3|西域试剂

Quisinostat dihydrochloride JNJ-26481585 dihydrochloride,98.28%

产品编号：Bellancom-15433A| CAS NO：875320-31-3| 分子式：C₂₁H₂₈Cl₂N₆O₂| 分子量：467.39

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货号	价格	库存与货期
Bellancom-15433A	￥1500.00	杭州北京（现货）
Bellancom-15433A	￥2400.00	杭州北京（现货）
Bellancom-15433A	￥7200.00	杭州北京（现货）

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Quisinostat dihydrochloride JNJ-26481585 dihydrochloride

产品介绍

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-HDAC inhibitor with IC₅₀s of 0.11 nM, 0.33 nM, 0.64 nM, 0.46 nM, and 0.37 nM for HDAC1, HDAC2, HDAC4, HDAC10 and HDAC11, respectively. Quisinostat dihydrochloride has a broad spectrum antitumoral activity.

体外研究

JNJ-26481585 inhibits HDAC isozymes in vitro.
JNJ-26481585 (30-1000 nM; 24 hours) is a potent pan-HDAC inhibitor in tumor cells.
JNJ-26481585 has broad spectrum antiproliferative activity against solid and hematologic cancer cell lines and induces apoptosis.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis

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.

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.
JNJ-26481585 induces continuous H3 acetylation in tumor tissue in vivo.
JNJ-26481585 (10 mg/kg; once daily; i.p.; for 14 days) strongly inhibits the growth of large pre-established HCT116 colon xenografts.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	NMRI nude mice, with HCT116 colon carcinoma cells xenografts
Dosage:	10 mg/kg
Administration:	Intraperitoneal injection, once daily, for 14 days
Result:	Strongly inhibited the growth of large pre-established HCT116 colon xenografts.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	NMRI nude mice, with HCT116 colon carcinoma cells xenografts
Dosage:	10 mg/kg
Administration:	Intraperitoneal injection, once daily, for 14 days
Result:	Strongly inhibited the growth of large pre-established HCT116 colon xenografts.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	NMRI nude mice, with HCT116 colon carcinoma cells xenografts
Dosage:	10 mg/kg
Administration:	Intraperitoneal injection, once daily, for 14 days
Result:	Strongly inhibited the growth of large pre-established HCT116 colon xenografts.

性状

Solid

溶解性数据

In Vitro:

DMSO : 31.25 mg/mL (66.86 mM; ultrasonic and warming and heat to 70°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 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。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in 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 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
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。