For research use only. Not for therapeutic Use.
CUDC-907 (Cat No.:I001301) is a potent inhibitor of histone deacetylase (HDAC) and phosphatidylinositol 3-kinase (PI3K). It exhibits dual inhibition of both HDAC and PI3K, targeting multiple signaling pathways involved in cancer progression. CUDC-907 has demonstrated antitumor activity in various cancer models, inhibiting cell proliferation and inducing apoptosis. It has shown efficacy against hematological malignancies and solid tumors in preclinical studies. The dual inhibition of HDAC and PI3K by CUDC-907 provides a unique approach to cancer therapy, making it a promising candidate for further investigation and potential clinical use.
| Catalog Number | I001301 |
| CAS Number | 1339928-25-4 |
| Synonyms | N-hydroxy-2-[[2-(6-methoxypyridin-3-yl)-4-morpholin-4-ylthieno[3,2-d]pyrimidin-6-yl]methyl-methylamino]pyrimidine-5-carboxamide |
| Molecular Formula | C23H24N8O4S |
| Purity | ≥95% |
| Target | HDAC |
| Solubility | DMSO 102 mg/mL; Water <1 mg/mL; Ethanol <1 mg/mL |
| Storage | 3 years -20C powder |
| IC50 | 1.7/5.0/1.8/2.8 nM (HDAC1/2/3/10); 19/54/39 nM (PI3Kα/β/δ) |
| IUPAC Name | N-hydroxy-2-[[2-(6-methoxypyridin-3-yl)-4-morpholin-4-ylthieno[3,2-d]pyrimidin-6-yl]methyl-methylamino]pyrimidine-5-carboxamide |
| InChI | InChI=1S/C23H24N8O4S/c1-30(23-25-11-15(12-26-23)22(32)29-33)13-16-9-17-19(36-16)21(31-5-7-35-8-6-31)28-20(27-17)14-3-4-18(34-2)24-10-14/h3-4,9-12,33H,5-8,13H2,1-2H3,(H,29,32) |
| InChIKey | JOWXJLIFIIOYMS-UHFFFAOYSA-N |
| SMILES | CN(CC1=CC2=C(S1)C(=NC(=N2)C3=CN=C(C=C3)OC)N4CCOCC4)C5=NC=C(C=N5)C(=O)NO |
| Reference | </br>1:Enhanced efficacy of 5-fluorouracil in combination with a dual histone deacetylase and phosphatidylinositide 3-kinase inhibitor (CUDC-907) in colorectal cancer cells. Hamam R, Ali D, Vishnubalaji R, Alsaaran ZF, Chalisserry EP, Alfayez M, Aldahmash A, Alajez NM.Saudi J Gastroenterol. 2017 Jan-Feb;23(1):34-38. doi: 10.4103/1319-3767.199136. PMID: 28139498 Free PMC Article</br>2:Dual HDAC and PI3K Inhibitor CUDC-907 Downregulates MYC and Suppresses Growth of MYC-dependent Cancers. Sun K, Atoyan R, Borek MA, Dellarocca S, Samson ME, Ma AW, Xu GX, Patterson T, Tuck DP, Viner JL, Fattaey A, Wang J.Mol Cancer Ther. 2017 Feb;16(2):285-299. doi: 10.1158/1535-7163.MCT-16-0390. Epub 2016 Dec 15. PMID: 27980108 </br>3:CUDC-907 Promotes Bone Marrow Adipocytic Differentiation Through Inhibition of Histone Deacetylase and Regulation of Cell Cycle. Ali D, Alshammari H, Vishnubalaji R, Chalisserry EP, Hamam R, Alfayez M, Kassem M, Aldahmash A, Alajez NM.Stem Cells Dev. 2017 Mar 1;26(5):353-362. doi: 10.1089/scd.2016.0183. Epub 2016 Nov 9. PMID: 27829312 </br>4:Safety, tolerability, and preliminary activity of CUDC-907, a first-in-class, oral, dual inhibitor of HDAC and PI3K, in patients with relapsed or refractory lymphoma or multiple myeloma: an open-label, dose-escalation, phase 1 trial. Younes A, Berdeja JG, Patel MR, Flinn I, Gerecitano JF, Neelapu SS, Kelly KR, Copeland AR, Akins A, Clancy MS, Gong L, Wang J, Ma A, Viner JL, Oki Y.Lancet Oncol. 2016 May;17(5):622-31. doi: 10.1016/S1470-2045(15)00584-7. Epub 2016 Mar 31. PMID: 27049457 </br>5:Human ATP-Binding Cassette Transporter ABCG2 Confers Resistance to CUDC-907, a Dual Inhibitor of Histone Deacetylase and Phosphatidylinositol 3-Kinase. Wu CP, Hsieh YJ, Hsiao SH, Su CY, Li YQ, Huang YH, Huang CW, Hsieh CH, Yu JS, Wu YS.Mol Pharm. 2016 Mar 7;13(3):784-94. doi: 10.1021/acs.molpharmaceut.5b00687. Epub 2016 Feb 2. PMID: 26796063 |
