1012054-59-9
CUDC-101
CAS: 1012054-59-9
Molecular Formula: C24H26N4O4
1012054-59-9 - Names and Identifiers
1012054-59-9 - Physico-chemical Properties
| Molecular Formula | C24H26N4O4 |
| Molar Mass | 434.49 |
| Density | 1.28 |
| Melting Point | 174-177℃ |
| Solubility | DMSO: soluble |
| Appearance | solid |
| Color | White or off-white |
| pKa | 9.47±0.20(Predicted) |
| Storage Condition | -20°C |
| Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month. |
| In vitro study | CUDC-101 as a specific inhibition of Class I and Class II HDACs family inhibitors, can not inhibit the third class HDACs family. CUDC-101 also has weak inhibitory activity against other protein kinases including KDR/VEGFR2, Lyn, Lck, Abl-1, FGFR-2, Flt-3 and Ret. The IC50 values were 0.85 μm, 0.84 μm, 5.91 μm, 2.89 μm, 3.43 μm, 1.5 μm and 3.2 μm, respectively. CUDC-101 exhibits a broad spectrum of anti-proliferative activity in many human cancer cells. The IC50 was between 0.04 μm and 0.80 μm. In many cancer cells, this activity even exceeds the inhibitory activity exhibited by erlotinib,lapatinib, and erlotinib and lapatinib when used together with vorinostat. CUDC-101 is able to inhibit the proliferative capacity of cancer cell lines with lapatinib and erlotinib resistance. CUDC-101 inhibition of erlotinib-resistant EGFR mutant T790M cell line, even if this inhibitory effect is not very complete, at the peak of its enzyme activity is still not more than 60%. In various cancer cell lines, CUDC-101 treatment not only increased the acetylation levels of histone H3 and H4 in a dose-dependent manner, but also increased the acetylation levels of the non-histone substrates p53 and α-tubulin. CUDC-101 can also inhibit the expression of HER3 in tumor cells, Met amplification and AKT reactivation. |
| In vivo study | CUDC-101 Hep-G2 liver tumor model treated with 120 mg/kg/day was able to induce tumor regression, compared to the maximum resistant dose of erlotinib (25 mg/kg/day) used and the inhibitory effect of vorinostat at an equimolar dose (72 mg/kg/day) was significantly effective. CUDC-101 inhibited the growth of erlotinib-sensitive H358 NSCLC xenografts in a dose-dependent manner. CUDC-101 also demonstrated the ability to inhibit the growth of erlotinib-sensitive A549 NSCLC xenografts. CUDC-101 showed significant promotion of tumor regression in both models, which were sensitive to lapatinib, A MDA-MB-468 breast tumor model with HER2 negative and EGFR overexpression and a CAL-27 brain neck cancer (HNSCC) model with EGFR overexpression. CUDC-101 inhibits tumor growth in HCT116 colon model with K-ras mutation and HPAC pancreatic tumor model with EGFR/HER2 (neu) expression. |
1012054-59-9 - Risk and Safety
| WGK Germany | 3 |
1012054-59-9 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.302 ml | 11.508 ml | 23.015 ml |
| 5 mM | 0.46 ml | 2.302 ml | 4.603 ml |
| 10 mM | 0.23 ml | 1.151 ml | 2.302 ml |
| 5 mM | 0.046 ml | 0.23 ml | 0.46 ml |
Last Update：2024-01-02 23:10:35
1012054-59-9 - Reference Information
| biological activity | CUDC-101 is a potent, multi-target inhibitor of HDAC,EGFR and HER2, the IC50 was 4.4 nM, 2.4 nM, and 15.7 nM, respectively, and inhibited type I/II HDACs, but did not inhibit type III, Sir-type HDACs. Phase 1. |
| Target | TargetValue EGFR (Cell-free assay) 2.4 nM HDAC (Cell-free assay) 4.4 nM HDAC1 (Cell-free assay) 4.5 nM HDAC6 (Cell-free assay) 5.1 nM HDAC3 (Cell-free assay) 9.1 nM |
| Target | Value |
| EGFR (Cell-free assay) | 2.4 nM |
| HDAC (Cell-free assay) | 4.4 nM |
| HDAC1 (Cell-free assay) | 4.5 nM |
| HDAC6 (Cell-free assay) | 5.1 nM |
| HDAC3 (Cell-free assay) | 9.1 nM |
| in vitro study | CUDC-101 as an inhibitor that specifically inhibits Class I and Class II HDACs family, cannot inhibit Class III HDACs family. CUDC-101 also has weak inhibitory activity against other protein kinases including KDR/VEGFR2, Lyn, Lck, Abl-1, FGFR-2, Flt-3 and Ret. The IC50 values were 0.85 μm, 0.84 μm, 5.91 μm, 2.89 μm, 3.43 μm, 1.5 μm and 3.2 μm, respectively. CUDC-101 exhibits a broad spectrum of anti-proliferative activity in many human cancer cells. The IC50 was between 0.04 μm and 0.80 μm. In many cancer cells, this activity even exceeds the inhibitory activity exhibited by erlotinib,lapatinib, and erlotinib and lapatinib when used together with vorinostat. CUDC-101 is able to inhibit the proliferative capacity of cancer cell lines with lapatinib and erlotinib resistance. CUDC-101 inhibition of erlotinib-resistant EGFR mutant T790M cell line, even if this inhibitory effect is not very complete, at the peak of its enzyme activity is still not more than 60%. In various cancer cell lines, CUDC-101 treatment not only increased the acetylation levels of histone H3 and H4 in a dose-dependent manner, but also increased the acetylation levels of the non-histone substrates p53 and α-tubulin. CUDC-101 can also inhibit the expression of HER3 in tumor cells, Met amplification and AKT reactivation. |
| in vivo study | CUDC-101 Hep-G2 liver tumor model treated with 120 mg/kg/day formula can induce tumor regression, the inhibitory effect was significantly more effective than at the maximum drug-resistant dose of erlotinib used (25 mg/kg/day) and at an equimolar dose of vorinostat (72 mg/kg/day). CUDC-101 inhibited the growth of erlotinib-sensitive H358 NSCLC xenografts in a dose-dependent manner. CUDC-101 also demonstrated the ability to inhibit the growth of erlotinib-sensitive A549 NSCLC xenografts. CUDC-101 showed significant promotion of tumor regression in both models, which were sensitive to lapatinib, A MDA-MB-468 breast tumor model with HER2 negative and EGFR overexpression and a CAL-27 brain neck cancer (HNSCC) model with EGFR overexpression. CUDC-101 inhibits tumor growth in HCT116 colon model with K-ras mutation and HPAC pancreatic tumor model with EGFR/HER2 (neu) expression. |
Last Update：2024-04-09 21:01:54
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Product Name: CUDC-101 Visit Supplier Webpage Request for quotation
CAS: 1012054-59-9
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 1012054-59-9
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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