1. Immunology/Inflammation NF-κB Metabolic Enzyme/Protease
  2. Reactive Oxygen Species
  3. CADD522

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。

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CADD522 Chemical Structure

CADD522 Chemical Structure

CAS No. : 199735-88-1

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Customer Review

MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CADD522 is a RUNX2-DNA binding inhibitor (downregulates RUNX2-mediated transcription of downstream target genes), with an IC50 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[1][2].

IC50 & Target[1]

RUNX2

10 nM ()

体外研究
(In Vitro)

CADD522 (0-100 μM; 24-72 h) 对 BC 细胞生长和存活表现出强烈的抑制作用[1]
CADD522 (50 μM;72 h) 通过诱导细胞周期停滞(G1 期)显示出抗增殖作用[1]
CADD522 (50 μM;8 days) 抑制肿瘤球形成和(50 μM;24 h)体外 BC 细胞侵袭(无细胞毒性[1]
CADD522 (2、10、25、50、100 μM;48 h) 通过抑制 T47D-RUNX2 和 T47D-Empty 细胞中的 RUNX2-DNA 结合来抑制 RUNX2 转录活性[1]
CADD522 (50 μM;72 h) 通过增加细胞中 RUNX2 的稳定性上调 RUNX2 水平[1]
/> CADD522 (50 μM;6 or 24 h) 增加 MCF7 和 MDA-468 细胞中线粒体的 ROS 生成[2]
CADD522 (0 -2000 nM,30 min) 抑制 MDA-231 和 MDA-468 细胞中的线粒体 ATP 合酶活性[2]

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

Cell Viability Assay[1]

Cell Line: MDA-MB-468, MCF7, MCF10A, IEC-6, GES-1 and C2C12 cells
Concentration: 0-100 μM
Incubation Time: 24-72 h
Result: Displayed a dose- and time-dependent cell growth inhibition over 72 h.
Exhibited low cytotoxicity for normal cell growth.

Cell Cycle Analysis[1]

Cell Line: MCF7, MDA-468 and MDA-231 cells
Concentration: 50 μM
Incubation Time: 72 h
Result: Induced MDA-231 cells accumulated at the G1 and G2/M phase whereas MCF7 and MDA-468 cells were at the G1 phase.

Cell Viability Assay[1]

Cell Line: MCF7, MCF7-tet-off cells
Concentration: 50 μM
Incubation Time: 8 days
Result: Dramatically decreased the size as well as the number of tumorspheres, and severely disrupted tumorspheres at day 4.
Showed a relatively selective effect on BC cells (did not have a significant influence on mammosphere formation of the MCF10A non-malignant mammary epithelial cells).

Cell Invasion Assay[1]

Cell Line: MCF7-tet-off (+Doxy), MCF7-tet-off (-Doxy) cells
Concentration: 50 μM
Incubation Time: 24 h
Result: Almost abrogated the invasiveness of both MCF7-tet-off (+Doxy) and MCF7-tet-off (-Doxy) cells without cellular toxicity.

Cell Viability Assay[1]

Cell Line: T47D-RUNX2 and T47D-Empty cells
Concentration: 2, 10, 25, 50, 100 μM
Incubation Time: 48 h
Result: Resulted in a dramatic decrease of the promoter-luciferase (Luc) activities of RUNX2 downstream target genes such as MMP13 and VEGF (metastasis markers) and OC (osteogenesis marker).

RT-PCR[1]

Cell Line: T47D and MCF7 cells (ectopic expressing RUNX2)
Concentration: 50 μM
Incubation Time: 72 h
Result: Significantly inhibited the mRNA level (RUNX2-mediated) of Glut-1 and LDHA.

Western Blot Analysis[1]

Cell Line: T47D-RUNX2 and MCF7-RUNX2 cells
Concentration: 50 μM
Incubation Time: 72 h
Result: Enhanced both mRNA and protein expression of RUNX2.

Western Blot Analysis[1]

Cell Line: MDA-468 and MDA-231 cells
Concentration: 50 μM
Incubation Time: 2, 4, 6 h
Result: Increased RUNX2 stability by delaying protein degradation.

Cell Viability Assay[2]

Cell Line: MCF7 and MDA-468 cells
Concentration: 50 μM
Incubation Time: 6 or 24 h
Result: Increased the level of mitochondrial ROS, which was more evident in serum-free than serum-containing condition.

Cell Viability Assay[2]

Cell Line: MDA-231 and MDA-468 cells
Concentration: 50, 250, 2000 nM (for MDA-231); 500, 2000 nM (for MDA-468)
Incubation Time: 30 min
Result: Inhibited the activity of A TP synthase.
体内研究
(In Vivo)

CADD522 (1、5 和 20 mg/kg;腹腔注射;每周两次,持续 45 天) 延缓肿瘤的发生并抑制小鼠肿瘤的生长[1]
CADD522 (10 mg/kg;腹腔注射;每周两次,持续 11 天) 抑制肿瘤转移并抑制小鼠 Ki-67 的表达[1]

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

Animal Model: Female mice (6-week-old; MMTV-PyMT transgenic model)[1].
Dosage: 1, 5 and 20 mg/kg
Administration: Intraperitoneal injection; twice a week for 45 days.
Result: Delayed the onset of the tumors, delayed tumor development and reduced tumor burden in transgenic MMTV-PyMT mice.
Reduced the tumor weight in mice.
Animal Model: Female NOD scid gamma (NSG) mice and nude mice (TNBC-PDX Br-001 model)[1].
Dosage: 10 mg/kg
Administration: Intraperitoneal injection; twice a week for 11 days.
Result: Significant decreased tumor volume and markedly inhibited expression of Ki-67.
Inhibited experimental metastasis of BC cells in vivo.(did not significantly decrease body weight or influence the general health of animals).
分子量

326.17

Formula

C15H13Cl2NO3

CAS 号
性状

固体

颜色

White to off-white

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, 2 years; -20°C, 1 year (stored under nitrogen)

溶解性数据
In Vitro: 

DMSO 中的溶解度 : 250 mg/mL (766.47 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.0659 mL 15.3294 mL 30.6589 mL
5 mM 0.6132 mL 3.0659 mL 6.1318 mL
查看完整储备液配制表

* 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, 2 years; -20°C, 1 year (stored under nitrogen)。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

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

  • 方案 一

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.17 mg/mL (6.65 mM); 澄清溶液

    此方案可获得 ≥ 2.17 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 21.7 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% Corn Oil

    Solubility: ≥ 2.17 mg/mL (6.65 mM); 澄清溶液

    此方案可获得 ≥ 2.17 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。

    1 mL 工作液为例,取 100 μL 21.7 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。

*In solvent : -80°C, 2 years; -20°C, 1 year (stored under nitrogen)

您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料
参考文献

完整储备液配制表

* 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, 2 years; -20°C, 1 year (stored under nitrogen)。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.0659 mL 15.3294 mL 30.6589 mL 76.6471 mL
5 mM 0.6132 mL 3.0659 mL 6.1318 mL 15.3294 mL
10 mM 0.3066 mL 1.5329 mL 3.0659 mL 7.6647 mL
15 mM 0.2044 mL 1.0220 mL 2.0439 mL 5.1098 mL
20 mM 0.1533 mL 0.7665 mL 1.5329 mL 3.8324 mL
25 mM 0.1226 mL 0.6132 mL 1.2264 mL 3.0659 mL
30 mM 0.1022 mL 0.5110 mL 1.0220 mL 2.5549 mL
40 mM 0.0766 mL 0.3832 mL 0.7665 mL 1.9162 mL
50 mM 0.0613 mL 0.3066 mL 0.6132 mL 1.5329 mL
60 mM 0.0511 mL 0.2555 mL 0.5110 mL 1.2775 mL
80 mM 0.0383 mL 0.1916 mL 0.3832 mL 0.9581 mL
100 mM 0.0307 mL 0.1533 mL 0.3066 mL 0.7665 mL
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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