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CUDC-101 CAS: 1012054-59-9

Category: Inhibitors
Product Name: CUDC-101
Cat No: I000119
CAS No: 1012054-59-9
Synonyms: 7-[4-(3-ethynylanilino)-7-methoxyquinazolin-6-yl]oxy-N-hydroxyheptanamide
Molecular Formula: C24H26N4O4
Molecular Weight: 434.5
SMILES: COC1=CC2=C(C(NC3=CC=CC(C#C)=C3)=NC=N2)C=C1OCCCCCCC(NO)=O
InChI: None
InChIKey: PLIVFNIUGLLCEK-UHFFFAOYSA-N
Solubility: DMSO ≥40mg/mL Water <1.2mg/mL Ethanol <1.2mg/mL
Target: HDAC
IC50: 4.4 nM(HDAC); 2.4 nM(EGFR); 15.7 nM(HER2)
Storage: powder
CAS 1012054-59-9,CUDC-101
  • Description

CUDC-101 is a potent multitargeted HDAC, EGFR and HER2 inhibitor with IC50 of 4.4, 2.4, and 15.7 nM, respectively.
IC50 Value: 4.4 nM(HDAC); 2.4 nM(EGFR); 15.7 nM(HER2)
Target: EGFR; HER2; HDAC
in vitro: CUDC-101 inhibits the erlotinib-resistant EGFR mutant T790M although its effects are incomplete with an Amax of ~60% of peak enzyme activity after inhibition. CUDC-101 treatment increases the acetylation of histone H3 and H4, as well as the acetylation of non-histone substrates of HDAC such as p53 and α-tubulin, in a dose-dependant manner in various cancer cell lines. CUDC-101 also suppresses HER3 expression, Met amplification, and AKT reactivation in tumor cells.
in vivo: Administration of CUDC-101 at 120 mg/kg/day induces tumor regression in the Hep-G2 liver cancer model, which is more efficacious than that of erlotinib at its maximum tolerated dose (25 mg/kg/day) and vorinostat at an equimolar concentration dose (72 mg/kg/day). CUDC-101 inhibits the growth of erlotinib-sensitive H358 NSCLC xenografts in a dose-dependent manner. CUDC-101 also shows potent inhibition of tumor growth in the erlotinib-resistant A549 NSCLC xenograft model. CUDC-101 produces significant tumor regression in the lapatinib-resistant, HER2-negative, EGFR-overexpressing MDA-MB-468 breast cancer model and the EGFR-overexpressing CAL-27 head and neck squamous cell carcinoma (HNSCC) model. Additionally, CUDC-101 inhibits tumor growth in the K-ras mutant HCT116 colorectal and EGFR/HER2 (neu)-expressing HPAC pancreatic cancer models.

  • Spec

Appearance:Solid powder
Purity: > 98%

  • References


1:CUDC-101, a Novel Inhibitor of Full-Length Androgen Receptor (flAR) and Androgen Receptor Variant 7 (AR-V7) Activity: Mechanism of Action and In Vivo Efficacy. Sun H, Mediwala SN, Szafran AT, Mancini MA, Marcelli M.Horm Cancer. 2016 Jun;7(3):196-210. doi: 10.1007/s12672-016-0257-2. Epub 2016 Mar 8. PMID: 26957440
2:Carfilzomib potentiates CUDC-101-induced apoptosis in anaplastic thyroid cancer. Zhang L, Boufraqech M, Lake R, Kebebew E.Oncotarget. 2016 Mar 29;7(13):16517-28. doi: 10.18632/oncotarget.7760. PMID: 26934320 Free PMC Article
3:Dual inhibition of HDAC and EGFR signaling with CUDC-101 induces potent suppression of tumor growth and metastasis in anaplastic thyroid cancer. Zhang L, Zhang Y, Mehta A, Boufraqech M, Davis S, Wang J, Tian Z, Yu Z, Boxer MB, Kiefer JA, Copland JA, Smallridge RC, Li Z, Shen M, Kebebew E.Oncotarget. 2015 Apr 20;6(11):9073-85. PMID: 25940539 Free PMC Article
4:A Phase I Study of CUDC-101, a Multitarget Inhibitor of HDACs, EGFR, and HER2, in Combination with Chemoradiation in Patients with Head and Neck Squamous Cell Carcinoma. Galloway TJ, Wirth LJ, Colevas AD, Gilbert J, Bauman JE, Saba NF, Raben D, Mehra R, Ma AW, Atoyan R, Wang J, Burtness B, Jimeno A.Clin Cancer Res. 2015 Apr 1;21(7):1566-73. doi: 10.1158/1078-0432.CCR-14-2820. Epub 2015 Jan 8. PMID: 25573383 Free Article
5:Human ATP-Binding Cassette transporters ABCB1 and ABCG2 confer resistance to CUDC-101, a multi-acting inhibitor of histone deacetylase, epidermal growth factor receptor and human epidermal growth factor receptor 2. Wu CP, Hsiao SH, Su CY, Luo SY, Li YQ, Huang YH, Hsieh CH, Huang CW.Biochem Pharmacol. 2014 Dec 15;92(4):567-76. doi: 10.1016/j.bcp.2014.10.003. Epub 2014 Oct 18. PMID: 25450670
6:Phase I first-in-human study of CUDC-101, a multitargeted inhibitor of HDACs, EGFR, and HER2 in patients with advanced solid tumors. Shimizu T, LoRusso PM, Papadopoulos KP, Patnaik A, Beeram M, Smith LS, Rasco DW, Mays TA, Chambers G, Ma A, Wang J, Laliberte R, Voi M, Tolcher AW.Clin Cancer Res. 2014 Oct 1;20(19):5032-40. doi: 10.1158/1078-0432.CCR-14-0570. Epub 2014 Aug 8. PMID: 25107918 Free Article
7:Novel (64)Cu-Labeled CUDC-101 for in Vivo PET Imaging of Histone Deacetylases. Meng Q, Li F, Jiang S, Li Z.ACS Med Chem Lett. 2013 Jul 25;4(9):858-62. doi: 10.1021/ml400191z. eCollection 2013 Sep 12. PMID: 24900760 Free PMC Article
8:Determination of CUDC-101 in rat plasma by liquid chromatography mass spectrometry and its application to a pharmacokinetic study. Zhang Q, Wen C, Xiang Z, Ma J, Wang X.J Pharm Biomed Anal. 2014 Mar;90:134-8. doi: 10.1016/j.jpba.2013.11.031. Epub 2013 Dec 4. PMID: 24366214
9:CUDC-101, a histone deacetylase inhibitor, improves the in vitro and in vivo developmental competence of somatic cell nuclear transfer pig embryos. Jin JX, Li S, Hong Y, Jin L, Zhu HY, Guo Q, Gao QS, Yan CG, Kang JD, Yin XJ.Theriogenology. 2014 Mar 1;81(4):572-8. doi: 10.1016/j.theriogenology.2013.11.011. Epub 2013 Nov 21. PMID: 24342668
10:Potential advantages of CUDC-101, a multitargeted HDAC, EGFR, and HER2 inhibitor, in treating drug resistance and preventing cancer cell migration and invasion. Wang J, Pursell NW, Samson ME, Atoyan R, Ma AW, Selmi A, Xu W, Cai X, Voi M, Savagner P, Lai CJ.Mol Cancer Ther. 2013 Jun;12(6):925-36. doi: 10.1158/1535-7163.MCT-12-1045. Epub 2013 Mar 27. PMID: 23536719 Free Article


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