Research Area
Product Type
United States ( Change Country )
CUDC-101 Chemical Structure
BIBW2992 (Afatinib)
BIBW2992 (Afatinib, Tomtovok, Tovok) irreversibly inhibits EGFR/HER2 including EGFRwt, EGFR L858R , EGFR L858R/T790M and HER2 with IC50 of 0.5 nM, 0.4 nM, 10 nM, 14 nM, respectively.
CI-1033 (Canertinib)
CI-1033 is a potent tyrosine kinase inhibitor of EGFR and erbB2 with IC50 of 1.5 nM and 9.0 nM, respectively.
Erlotinib HCl
Erlotinib HCl also known as Tarceva, CP-358774, OSI-774, NSC-718781 is a HCL salt with IC50 of 2 nM for HER1/EGFR TK.
Gefitinib (Iressa)
Gefitinib (Iressa) also known as ZD-1839 & Iressa is a novel potent EGFR tyrosine kinase & Akt phosphorylations inhibitor with IC50 of 37, 26 and 57 nM.
Lapatinib Ditosylate (Tykerb)
Lapatinib (Tyverb, GW-572016, GW-2016) is a potent purified EGFR and ErbB-2 inhibitor with IC50 of 10.2 and 9.8 nM, respectively.
LBH589 (Panobinostat)
LBH589 (Panobinostat) is a HDAC inhibitor, IC50 for inhibition of proliferation in MOLT-4 cells is approximately 5 μM and for Reh cells is approximately 20 μM.
Trichostatin A (TSA)
Inhibitor of HDAC, HDAC inhibitory activity of TSA was similar in all cell lines with mean ± SD IC50 of 2.4 ± 0.5 nm (range, 1.5–2.9 nm)
Vandetanib (Zactima)
Vandetanib (Zactima) is a VEGFR and EGFR antagonist and a tyrosine kinase inhibitor with IC50 of 60, 90, 40 nM for HUVEC proliferation, PC-9 cells and tyrosine kinase activity, respectively.
Vorinostat (SAHA)
Vorinostat also known as SAHA, Zolinza, MK-0683 is an HDAC inhibitor. Vorinostat CAS No 149647-78-9 with purity >99% & solubility DMSO is available.
MS-275 (Entinostat)
MS-275 (Entinostat) is a potent HDAC inhibitor with IC50 of 0.3 and 8µM for HDAC1 and HDAC3, respectively.
Biological Activity
CUDC-101 is a potent multitargeted HDAC, EGFR and HER2 inhibitor with IC50 of 4.4, 2.4, and 15.7 nM, respectively. CUDC-101 has novel structure incorporating HDAC inhibitory functionality into the pharmacophore of the EGFR and HER2 inhibitors. In most tumor cell lines tested, CUDC-101 exhibits efficient antiproliferative activity with greater potency than vorinostat (SAHA), erlotinib, lapatinib, and combinations of vorinostat/erlotinib and vorinostat/lapatinib. In vivo, CUDC-101 promotes tumor regression or inhibition in various cancer xenograft models including nonsmall cell lung cancer (NSCLC), liver, breast, head and neck, colon, and pancreatic cancers. [1][2]
References on CUDC-101
- [1] J. Med. Chem. 2010;3, 2000–2009
- [2] Cancer Res 2010;70:3647-3656
Product Information
| Molecular Weight (WM): | 434.49 |
|---|---|
| Formula: | C24H26N4O4 |
| CAS No.: | 1012054-59-9 |
| Synonyms: |
N/A
|
| Dissolve in (25°C): | DMSO ≥43mg/mL |
| Water <1mg/mL | |
| Ethanol <1mg/mL | |
| Storage: | 2 years-20°CPowder |
| 1 week-4°Cin DMSO | |
| 1 month-80°in DMSO |
Quality Control & MSDS
Research Area
Receptor Tyrosine Kinase >> EGFR >> EGFR Inhibitors
Angiogenesis >> EGFR >> EGFR Inhibitors
JAK / STAT >> EGFR >> EGFR Inhibitors
Receptor Tyrosine Kinase >> HER2 >> HER2 Inhibitors
Angiogenesis >> HER2 >> HER2 Inhibitors
HDAC-HSP-Aurora >> HDAC >> HDAC Inhibitors
NF-κB Pathway >> HDAC >> HDAC Inhibitors
Angiogenesis >> EGFR >> EGFR Inhibitors
JAK / STAT >> EGFR >> EGFR Inhibitors
Receptor Tyrosine Kinase >> HER2 >> HER2 Inhibitors
Angiogenesis >> HER2 >> HER2 Inhibitors
HDAC-HSP-Aurora >> HDAC >> HDAC Inhibitors
NF-κB Pathway >> HDAC >> HDAC Inhibitors
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Click to enlarge
After starved in serum-free medium for 24h, Breast cancer cells incubated with the indicated concentrations of CUDC-101 for 3h,followed by 15-minute stimolation of 100ng/ml EGF
After starved in serum-free medium for 24h, Breast cancer cells incubated with the indicated concentrations of CUDC-101 for 3h,followed by 15-minute stimolation of 100ng/ml EGF
Data independently produced by Dr Zhang of Tianjin Medical University CUDC-101 purchased from Selleck
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Click to enlarge
Effect of CUDC-101 on the viability was detected by WST-1 method after 3 days treatment in endometrial cancer cell line Hec50 and lshikawa and ovarian cancer cell line SKOV3,Caov and PA-1.
Effect of CUDC-101 on the viability was detected by WST-1 method after 3 days treatment in endometrial cancer cell line Hec50 and lshikawa and ovarian cancer cell line SKOV3,Caov and PA-1.
Data independently produced by Dr Xiangbing Meng of University of Iowa CUDC-101 purchased from Selleck
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After starved in serum-free medium for 24h, Breast cancer cells incubated with the indicated concentrations of CUDC-101 for 3h,followed by 15-minute stimolation of 100ng/ml EGF
|
Data independently produced by Dr Zhang of Tianjin Medical University
Effect of CUDC-101 on the viability was detected by WST-1 method after 3 days treatment in endometrial cancer cell line Hec50 and lshikawa and ovarian cancer cell line SKOV3,Caov and PA-1.
|
Data independently produced by Dr Xiangbing Meng of University of Iowa
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