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CAS No.: 199735-88-1

CADD522 Catalog No. CSN25632

Synonyms: MFCD00167693

CADD522 is a small molecule that inhibits the DNA binding of RUNX2. It negatively regulated transcription of RUNX2 target genes such as matrix metalloproteinase-13, vascular endothelial growth factor and glucose transporter-1, but upregulated RUNX2 expression by increasing RUNX2 stability. CADD522 may represent a potential antitumor drug.

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技术信息

生物活性

描述The runt-related transcription factor-2 (RUNX2) promotes breast cancer (BC) progression and metastasis through transcriptional activation of its target genes. CADD522 is identified as a novel inhibitor of RUNX2-DNA binding with an IC₅₀ of 10 nM. CADD522 inhibited the DNA binding activity of all RUNX proteins, but most prominent inhibition was observed for RUNX2-DNA binding. CADD522 also inhibited RUNX2 binding to the MMP13 (a well-known RUNX2 target gene) oligonucleotides in a dose-dependent manner. CADD522 significantly inhibited RUNX2 enrichment in the MCF7-RUNX2 cells. CADD522 (0 ∼ 100 μM) displayed a dose- and time-dependent cell growth inhibition over 72 hrs. However, the sensitivity of non-malignant cells to CADD522 was much lower than that of BC cell lines, indicating that CADD522 might not exhibit serious cytotoxicity for normal cell growth. CADD522 at 50 μM for 72 hrs exerted mild but significant growth inhibition (< 50%) in the majority of TNBC and luminal type BC cells. Among them, MDA-MB-468 (MDA-468) cells were most sensitive to CADD522 (> 50%). Moreover, this CADD522 treatment increased cell populations at the G1 phase with reduction at the S phase, indicating that the anti-proliferative effect of CADD522 might be associated with cell cycle arrest. Further, CADD522 dramatically decreased the size as well as the number of tumorspheres and tumorspheres were severely disrupted a few days after CADD522 treatment at the initial day of cell plating. In vivo, the intraperitoneal (i.p.) administration of CADD522 into the MMTV-PyMT mice (up to 20 mg/kg) delayed tumor development and reduced tumor burden in transgenic MMTV-PyMT mice^[1].
参考文献

[1] Kim MS, Gernapudi R, Choi EY, Lapidus RG, Passaniti A. Characterization of CADD522, a small molecule that inhibits RUNX2-DNA binding and exhibits antitumor activity. Oncotarget. 2017;8(41):70916-70940

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.0658 mL
- 15.3292 mL
- 30.6584 mL
- 5 mM
- 0.6132 mL
- 3.0658 mL
- 6.1317 mL
- 10 mM
- 0.3066 mL
- 1.5329 mL
- 3.0658 mL

技术信息

CAS号

199735-88-1

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C15H13Cl2NO3

运输

蓝冰

分子量

326.17

别名

MFCD00167693

溶解度

DMSO	65.0 mg/mL (199.3 mM)
Water	Insoluble
Ethanol	65.0 mg/mL (199.3 mM)

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CADD522 Catalog No. CSN25632

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