CADD522

目录号: PL10932 纯度: ≥98%
CADD522 是一种 RUNX2-DNA 结合抑制剂 (下调 RUNX2 介导的下游靶基因的转录),其 IC50 值为 10 nM。CADD522 还可通过增加线粒体驱动的细胞 ROS 水平发挥其抗肿瘤活性。CADD522 能抑制体内原发肿瘤的生长和免疫受损小鼠肺部肿瘤细胞的实验性转移,可用于癌症的研究。
CAS No. :199735-88-1
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中文名称
CADD522
英文名称
CADD522
英文别名
3-([(3,4-Dichlorophenyl)amino]carbonyl)bicyclo[2.2.1]hept-5-ene-2-carboxylic acid;CADD522;3-[(3,4-dichlorophenyl)carbamoyl]bicyclo[2.2.1]hept-5-ene-2-carboxylic acid;3-{[(3,4-Dichlorophenyl)amino]carbonyl}bicyclo[2.2.1]hept-5-ene-2-carboxylic acid;MLS001212609;HMS2815M08;STK493580;3-(3,4-Dichloro-phenylcarbamoyl)-bicyclo[2.2.1]hept-5-ene-2-carboxylic acid;SMR000514886
Cas No.
199735-88-1
分子式
C15H13Cl2NO3
分子量
326.17
包装储存
4°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
详情描述
CADD522 是一种 RUNX2-DNA 结合抑制剂 (下调 RUNX2 介导的下游靶基因的转录),其 IC50 值为 10 nM。CADD522 还可通过增加线粒体驱动的细胞 ROS 水平发挥其抗肿瘤活性。CADD522 能抑制体内原发肿瘤的生长和免疫受损小鼠肺部肿瘤细胞的实验性转移,可用于癌症的研究。
产品详情
CADD522 是一种 RUNX2-DNA 结合抑制剂 (下调 RUNX2 介导的下游靶基因的转录),其 IC50 值为 10 nM。CADD522 还可通过增加线粒体驱动的细胞 ROS 水平发挥其抗肿瘤活性。CADD522 能抑制体内原发肿瘤的生长和免疫受损小鼠肺部肿瘤细胞的实验性转移,可用于癌症的研究。
生物活性
CADD522 is a RUNX2-DNA binding inhibitor (downregulates RUNX2-mediated transcription of downstream target genes), with an IC 50 of 10 nM. CADD522 inhibits primary tumor growth and experimental metastasis of tumor cells in the lungs of immune-compromised mice. CADD522 can be used in study of cancer.
性状
Solid
IC50 & Target[1][2]
RUNX2-DNA binding
体外研究(In Vitro)
CADD522 (0-100 μM; 24-72 h) exhibits a strong inhibitory effect on BC cell growth and survival.
CADD522 (50 μM; 72 h) shows anti-proliferative effect by inducing cell cycle arrest (G1 phase).
CADD522 (50 μM; 8 days) inhibits tumorsphere formation and (50 μM; 24 h) in vitro invasion of BC cells (without cellular toxicity).
CADD522 (2, 10, 25, 50, 100 μM; 48 h) inhibits RUNX2 transcriptional activity by inhibiting RUNX2-DNA binding in T47D-RUNX2 and T47D-Empty cells.
CADD522 (50 μM; 72 h) upregulates RUNX2 levels through increased RUNX2 stability in cells.
CADD522 (50 μM; 6 or 24 h) increases ROS generation of mitochondrial in MCF7 and MDA-468 cells.
CADD522 (0-2000 nM, 30 min) inhibits mitochondrial ATP synthase activity in MDA-231 and MDA-468 cells. has not independently confirmed the accuracy of
体内研究(In Vivo)
CADD522 (1, 5 and 20 mg/kg; i.p.; twice a week for 45 days) delays the onset of the tumors and suppresses tumor growth in mice.
CADD522 (10 mg/kg; i.p.; twice a week for 11 days) suppresses tumor metastasis and inhibits expression of Ki-67 in mice. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
参考文献
[1]. Kim MS, et al. Characterization of CADD522, a small molecule that inhibits RUNX2-DNA binding and exhibits antitumor activity. Oncotarget. 2017 Aug 10;8(41):70916-70940.
[2]. Kim MS, et al. Targeting breast cancer metabolism with a novel inhibitor of mitochondrial ATP synthesis. Oncotarget. 2020 Oct 27;11(43):3863-3885.
溶解度数据
In Vitro: DMSO : 250 mg/mL (766.47 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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