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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C23H24N8O4S |
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分子量 | 508.55 | CAS No. | 1339928-25-4 | |
Solubility (25°C)* | 体外 | DMSO | 100 mg/mL (196.63 mM) | |
Water | Insoluble | |||
Ethanol | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | CUDC-907 is a dual PI3K and HDAC inhibitor for PI3Kα and HDAC1/2/3/10 with IC50 of 19 nM and 1.7 nM/5 nM/1.8 nM/2.8 nM, respectively. CUDC-907 induces cell cycle arrest and apoptosis in breast cancer cells. Phase 1. |
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in vitro | CUDC-907 inhibits other PI3K isoforms such as PI3Kβ, PI3Kγ, PI3Kδ, PI3KɑH1047R and PI3KɑE545K with IC50 of 54 nM, 311 nM, 39 nM, 73 nM and 62 nM, respectively. Moreover, CUDC-907 also prevents HDAC subtypes HDAC8, HDAC6 and HDAC11 with IC50 of 191 nM, 27 nM and 5.4 nM, respectively. [1] In addition, CUDC-907 suppresses other types of HDAC enzymatic activity with lower potency. CUDC-907 inhibits the growth of a series of B cell lymphoma such as Granta 519, DOHH2, RL, Pfeiffer, SuDHL4, Daudi and Raji with IC50 of 7 nM, 1 nM, 2 nM, 4 nM, 3 nM, 15 nM and 9 nM, respectively. CUDC-907 also blocks the proliferation of Myeloma including RPMI8226, OPM-2 and ARH77 with IC50 of 2 nM, 1 nM and 5 nM, respectively. CUDC-907 displays greater anti-tumor activity in multiple myeloma and B cell lymphoma. [1] |
in vivo | CUDC-907 has a long half-life in murine tumors. CUDC-907 induces apoptosis and inhibits cancer cell proliferation in xenograft tumors. [1] In efficacy studies in NHL and MM models, CUDC-907 is more efficacious than either a single-agent PI3K or HDAC inhibitor reference compound or a combination of the two agents given at maximally tolerated doses (MTD). Furthermore, CUDC-907 is more efficacious than the PI3Kδ-selective inhibitor CAL-101 when dosed at MTD doses. [1] |
細胞アッセイ | 細胞株 | Cell-free assays |
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濃度 | IC50 of 1.7, 5, 1.8, 2.8, 19, 54, and 39 nM for HDAC1, HDAC2, HDAC3, HDAC10, PI3Kα, PI3Kβ, and PI3Kδ respectively | |
反応時間 | ||
実験の流れ | ||
動物実験 | 動物モデル | NHL and MM models in mice |
投薬量 | 100 mg/kg | |
投与方法 | Administered via p.o. |
Data from [Data independently produced by , , Stem Cells Dev, 2017, 26(5):353-362]
Data from [Data independently produced by , , Saudi J Gastroenterol, 2017, 23(1):34-38]
Reversible epigenetic alterations mediate PSMA expression heterogeneity in advanced metastatic prostate cancer [ JCI Insight, 2023, 8(7)e162907] | PubMed: 36821396 |
Anti-tumor effects of dual PI3K-HDAC inhibitor CUDC-907 on activation of ROS-IRE1α-JNK-mediated cytotoxic autophagy in esophageal cancer [ Cell Biosci, 2022, 12(1):135] | PubMed: 35989326 |
Co-targeting of HDAC, PI3K, and Bcl-2 results in metabolic and transcriptional reprogramming and decreased mitochondrial function in acute myeloid leukemia [ Biochem Pharmacol, 2022, 205:115283] | PubMed: 36208684 |
Utilizing an Endogenous Progesterone Receptor Reporter Gene for Drug Screening and Mechanistic Study in Endometrial Cancer [ Cancers (Basel), 2022, 14(19)4883] | PubMed: 36230806 |
Histone Deacetylase Inhibitors as a Therapeutic Strategy to Eliminate Neoplastic "Stromal" Cells from Giant Cell Tumors of Bone [ Cancers (Basel), 2022, 14(19)4708] | PubMed: 36230631 |
poly(I:C) synergizes with proteasome inhibitors to induce apoptosis in cervical cancer cells [ Transl Oncol, 2022, 18:101362] | PubMed: 35151092 |
The combination of CUDC-907 and gilteritinib shows promising in vitro and in vivo antileukemic activity against FLT3-ITD AML [ Blood Cancer J, 2021, 11(6):111] | PubMed: 34099621 |
Targeting phosphoinositide 3-kinases and histone deacetylases in multiple myeloma [ Exp Hematol Oncol, 2021, 10(1):19] | PubMed: 33663586 |
Antitumor activity and mechanism of resistance of the novel HDAC and PI3K dual inhibitor CUDC-907 in pancreatic cancer [ Cancer Chemother Pharmacol, 2021, 10.1007/s00280-020-04210-0] | PubMed: 33392641 |
The HDAC and PI3K Dual Inhibitor CUDC-907 Synergistically Enhances the Antileukemic Activity of Venetoclax in Preclinical Models of Acute Myeloid Leukemia [ Haematologica, 2020, 12;haematol.2019.233445] | PubMed: 32165486 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
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