上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。
Dacinostat (Synonyms: NVP-LAQ824; LAQ824) 纯度: 98.45%
Dacinostat 是一种有效的 HDAC 抑制剂,IC50 值为 32 nM;Dacinostat 同时可抑制 HDAC1 的活性,IC50 值为 9 nM,主要用于癌症研究。
Dacinostat Chemical Structure
CAS No. : 404951-53-7
规格 | 价格 | 是否有货 | 数量 |
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Free Sample (0.1-0.5 mg) | Apply now | ||
10 mM * 1 mL in DMSO | ¥2380 | In-stock | |
10 mg | ¥2160 | In-stock | |
50 mg | ¥5760 | In-stock | |
100 mg | 询价 | ||
200 mg | 询价 |
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Dacinostat 相关产品
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生物活性 |
Dacinostat is a potent HDAC inhibitor, with an IC50 of 32 nM; Dacinostat also inhibits HDAC1 with an IC50 of 9 nM, and used in cancer research. |
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IC50 & Target |
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体外研究 (In Vitro) |
Dacinostat (NVP-LAQ824) activates p21 promoter, with AC50 of 0.30 μM. NVP-LAQ824 inhibits tumor cell (H1299, HCT116) growth, with IC50s of 150 and 10 nM, respectively. NVP-LAQ824 also shows inhibitory activities against two prostate cancer cell lines (DU145 and PC3) and a breast cancer line (MDA435), with IC50s of 18, 23, 39 nM, respectively. Continuous exposure of NVP-LAQ824 for 72 h produces LD90s of 0.09 M in HCT116 cells and 0.47 M in A549 cells. NVP-LAQ824 treatment of NDHF cells causes the expected G1-S growth arrest in addition to a significant reduction of cells in S-phase and accumulation of cells at the G2-M checkpoint. NVP-LAQ824 induces apoptotic death in human tumor cells. NPV-LAQ824 increases acetylation of histones H3 and H4[1]. Dacinostat inhibits HDAC1 with an IC50 of 9 nM[2]. Dacinostat (10 and 20 nM) suppresses proliferation of AML fusion protein-expressing 32D cells. Dacinostat impairs short-term engraftment potential of leukemic stem cells. Dacinostat exhausts in vitro self-renewal potential of murine AML1/ETO- and PLZF/RARα-positive HSC[3]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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体内研究 (In Vivo) |
NVP-LAQ824 produces a dose-dependent inhibition of tumor growth, and at 100 mg/kg, its antitumor effect is similar to that of 5-Fluorouracil[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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分子量 |
379.45 |
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Formula |
C22H25N3O3 |
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CAS 号 |
404951-53-7 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
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溶解性数据 |
In Vitro:
DMSO : ≥ 43 mg/mL (113.32 mM) * “≥” means soluble, but saturation unknown. 配制储备液
*
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。 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
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参考文献 |
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Kinase Assay [2] |
The HDAC enzymatic assay measures compound activity in inhibiting purified HDAC isoforms. HDACs 1, 3, and 6 are immunopurified from 293 cells stably expressing the FLAG-tagged HDAC isoform, whereas HDACs 2, 4, 5, 7, 8, 9, 10, and 11 are purified from the baculovirus expression system. HDAC activity is measured in a fluorescent assay in which deacetylation of the substrate, bis-Boc-(Ac)Lys-rhodamine 110, generates a fluorophore that can be detected on a fluorometric plate reader[2]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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Cell Assay [2] |
Cells are plated at 5000−10000 cells per well in 96-well plates and treated with eight serial compound dilutions. Cell viability following 72 h of compound treatment is measured using the CellTiter-Glo or MTS assay. XLfit 4 is used for plotting of the growth curves and calculation of IC50 values[2]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
Animal Administration [1] |
The studies are performed on-site, using outbred athymic (nu/nu) female mice. Mice are anesthetized with Metofane, and a cell suspension (100 μL) containing 1×106 HCT116 cells is injected s.c. into the right axillary (lateral) region of each animal. Tumors are allowed to reach the volume of approximately 100-400 mm3. At this point, mice bearing tumors with acceptable morphology (non-necrotic) and of similar size range are selected and distributed into groups of six for the studies. NVP-LAQ824 is dissolved in DMSO to create a stock solution, which is further diluted just before dosing with D5W to a final DMSO concentration of 10%. Tumor-bearing mice are treated with the compound by i.v. injection into the tail vein. NVP-LAQ824 is dosed once daily, 5 days/week, for a total of 15 doses. 5-Fluorouracil is administered at 100 mg/kg in 0.9% saline 1 day/week for a total of three doses. The control groups are treated with the vehicle. Tumors are collected from the animals at the indicated time points[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
参考文献 |
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