J22352|cas:2252395-44-9|西域试剂

J22352,98.72%

产品编号：Bellancom-126147| CAS NO：2252395-44-9| 分子式：C₂₄H₂₁N₃O₄| 分子量：415.44

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货号	价格	库存与货期
Bellancom-126147	￥1200.00	杭州北京（现货）
Bellancom-126147	￥1900.00	杭州北京（现货）
Bellancom-126147	￥5500.00	杭州北京（现货）
Bellancom-126147	￥9400.00	杭州北京（现货）

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J22352

产品介绍

J22352 是一种具有类似靶向嵌合体蛋白水解 (PROTAC) 特性、高度选择性 HDAC6 抑制剂，其 IC₅₀ 值为 4.7 nM，J22352 通过抑制胶质母细胞瘤自噬、诱发抗肿瘤免疫反应来促进 HDAC6 降解和诱导抗癌效果，并通过降低 PD-L1 的免疫抑制活性，使宿主抗肿瘤活性恢复。

生物活性

J22352 is a PROTAC (proteolysis-targeting chimeras)-like and highly selective HDAC6 inhibitor with an IC₅₀ value of 4.7 nM. J22352 promotes HDAC6 degradation and induces anticancer effects by inhibiting autophagy and eliciting the antitumor immune response in glioblastoma cancers, and leading to the restoration of host antitumor activity by reducing the immunosuppressive activity of PD-L1.

体外研究

J22352 (0.1-20 μM; 72 hours) decreases U87MG cell viability in a dose-dependent manner.
J22352 (10 μM; 24 hours) shows a dose-dependent decrease in HDAC6 protein abundance.

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

Cell Viability Assay

Cell Line:	U87MG cells
Concentration:	0.1 μM; 0.5 μM; 1μM; 2.5 μM; 5 μM; 10 μM; 20 μM
Incubation Time:	72 hours
Result:	A dose-dependent decrease on U87MG cell proliferation.

Western Blot Analysis

Cell Line:	U87MG cells
Concentration:	10 μM
Incubation Time:	24 hours
Result:	A dose-dependent decrease in aberrant overexpression of HDAC6 in glioblastoma.

体内研究
(In Vivo)

J22352 (10 mg/kg; given i.p. per day for 14 days in male nude mice) results in a >80% tumor growth inhibition (TGI) rate. J22352 is well tolerated in mice.

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

Animal Model:	Male nude mice (BALB/cAnN.Cg-Foxnlnu/CrlNarl, 4-6 weeks old)
Dosage:	10 mg/kg
Administration:	Given i.p.; per day for 14 days
Result:	Marked anti-tumor effects and well tolerated in mice.

体内研究

J22352 (10 mg/kg; given i.p. per day for 14 days in male nude mice) results in a >80% tumor growth inhibition (TGI) rate. J22352 is well tolerated in mice.

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

Animal Model:	Male nude mice (BALB/cAnN.Cg-Foxnlnu/CrlNarl, 4-6 weeks old)
Dosage:	10 mg/kg
Administration:	Given i.p.; per day for 14 days
Result:	Marked anti-tumor effects and well tolerated in mice.

体内研究

J22352 (10 mg/kg; given i.p. per day for 14 days in male nude mice) results in a >80% tumor growth inhibition (TGI) rate. J22352 is well tolerated in mice.

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

Animal Model:	Male nude mice (BALB/cAnN.Cg-Foxnlnu/CrlNarl, 4-6 weeks old)
Dosage:	10 mg/kg
Administration:	Given i.p.; per day for 14 days
Result:	Marked anti-tumor effects and well tolerated in mice.

性状

Solid

溶解性数据

In Vitro:

DMSO : 125 mg/mL (300.89 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.4071 mL	12.0354 mL	24.0709 mL
5 mM	0.4814 mL	2.4071 mL	4.8142 mL
10 mM	0.2407 mL	1.2035 mL	2.4071 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。-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 (5.01 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.01 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 (5.01 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.01 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 (5.01 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.01 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。