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Tubulin/HDAC-IN-1

产品编号 T61524 CAS 2413587-26-3

Tubulin/HDAC-IN-1 is a compound that functions as a dual inhibitor for tubulin and HDAC-IN-1. It achieves this by interacting with tubulin through CH/π interaction and with HDAC8 through hydrogen bond interaction. This compound effectively inhibits tubulin polymerization and selectively targets HDAC8 with an IC50 of 150 nM. Additionally, Tubulin/HDAC-IN-1 demonstrates cytotoxicity against various human cancer cells, induces cell cycle arrest in the G2/M phase, and triggers cell apoptosis. This compound is valuable for studying hematologic and solid tumors, including neuroblastoma and leukemia [1].

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Tubulin/HDAC-IN-1, CAS 2413587-26-3

规格	价格/CNY	货期
25 mg	￥ 10,600	6-8周
50 mg	￥ 13,800	6-8周
100 mg	￥ 17,500	6-8周

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生物活性

化学信息

存储 & 溶解度

产品描述	Tubulin/HDAC-IN-1 is a compound that functions as a dual inhibitor for tubulin and HDAC-IN-1. It achieves this by interacting with tubulin through CH/π interaction and with HDAC8 through hydrogen bond interaction. This compound effectively inhibits tubulin polymerization and selectively targets HDAC8 with an IC50 of 150 nM. Additionally, Tubulin/HDAC-IN-1 demonstrates cytotoxicity against various human cancer cells, induces cell cycle arrest in the G2/M phase, and triggers cell apoptosis. This compound is valuable for studying hematologic and solid tumors, including neuroblastoma and leukemia [1].
体外活性	Tubulin/HDAC-IN-1 (Compound 12a, 72 h) shows cytotoxicity against various human cancer cell lines with an averaged IC 50 value of 0.6 nM [1]. Tubulin/HDAC-IN-1 (2 nM, 24 h) induces HT29 cell cycle arrest in the G2/M phase and produces caspase-induced apoptosis of HT29 cells through mitochondrial dysfunction [1]. Tubulin/HDAC-IN-1 selectively inhibits HDAC8 (IC 50 : 150 nM), inhibits HDAC6 and HDAC11 with IC 50 values of 1 μM and 1.9 μM respectively [1]. Tubulin/HDAC-IN-1 (0.5-100 nM, 24 h/30 min) dose-dependently increases γH2AX level and acetylated SMC3 in HT-29 cells [1]. Tubulin/HDAC-IN-1 (5-15 μΜ, 0-40 min) inhibits tubulin polymerization in a dose-dependent manner, with a maximal effect achieved at 10 μM [1]. Tubulin/HDAC-IN-1 (250 nM, 30 min) depolymerizes the cell microtubule network, and the effect is not specific [1]. Tubulin/HDAC-IN-1 shows good in vitro metabolic stability expressed by the intrinsic clearance CLint (given in μL/min/mg protein) using rat liver microsomes (RLM) and human liver microsomes (HLM) [1]. Compound RLM RLM HLM HLM t 1/2 (h) CL int t 1/2 CL int Tubulin/HDAC-IN-1 6.6 1.75 32 0.36 Cell Proliferation Assay [1] Cell Line: Various tumor cell lines as below Concentration: Incubation Time: 72 h Result: Activities of Tubulin/HDAC-IN-1 (Compound 12a) against various tumor cell lines (IC 50 nM): NCIN87 K562 K562R MiaPaca2 SKOV3 A549 MCF-7 MDA-MB-231 HCT116 HT-29 Tubulin/HDAC-IN-1 0.1 0.35 0.56 0.94 0.6 0.84 0.78 0.7 0.6 0.62 Western Blot Analysis [1] Cell Line: HT-29 cells Concentration: 0.5, 1, 5, 10 nM for γH2AX; 0.5, 1, 100 nM for acetylated SMC3 Incubation Time: 24 h for γH2AX, 30 min for acetylated SMC3 Result: Dose-dependently increased γH2AX level and acetylated SMC3.
体内活性	Tubulin/HDAC-IN-1 (Compound 12a, intratumoral injection, 0.25 mg/kg, three times a week for two weeks) decreases MCA205 tumor growth and extends the overall survival of treated mice in allogeneic sarcoma mice model [1]. Animal Model: Allogeneic sarcoma model in C57BL/6 mice [1] Dosage: 0.1, 0.25, 0.50 mg/kg, three times a week for two weeks. Administration: Intratumoral injection Result: Decreased tumor growth and extended the overall survival of treated mice with no obvious side effects.

分子量	374.39
分子式	C21H18N4O3
CAS No.	2413587-26-3

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

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