受注:045-509-1970 |
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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder | |
化学式 | C25H27N3O5 |
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分子量 | 449.50 | CAS No. | 1323403-33-3 | |
Solubility (25°C)* | 体外 | DMSO | 90 mg/mL (200.22 mM) | |
Ethanol | 5 mg/mL (11.12 mM) | |||
Water | 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 | Iberdomide (CC-220) is a novel oral immunomodulatory compound that targets cereblon, part of the CRL4CRBN E3 ubiquitin ligase complex, with an IC50 of 60 nM in a competitive TR-FRET assay. Iberdomide (CC-220) induces apoptosis with antitumor and immunostimulatory activities. |
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in vitro | In cellular degradation assays, treatment with CC-220 results in the loss of Ikaros protein levels with an EC50 of 1 nM. CC-220 is similarly potent toward Aiolos, with an EC50 of 0.5 nM[1]. CC-220 is a potent anti-proliferative and pro-apoptotic compound that shows activity in several MM cell line categories. CC-220 induces PBMC-mediated killing of all MM cell lines regardless of the level of Cereblon expression and cell autonomous sensitivity. CC-220 acts through binding of Cereblon, leading to the degradation of the hematopoietic transcription factors Ikaros and Aiolos, followed by disruption of the MM promoting c-Myc/IRF4 axis[2]. |
細胞アッセイ | 細胞株 | DF15 cells |
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濃度 | 60 nM | |
反応時間 | 5 h | |
実験の流れ | Cells were treated with CC-220 for 5 h before harvest. |
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動物実験 | 動物モデル | Transgenic mice |
投薬量 | 10 mg/kg | |
投与方法 | o.g. |
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Degradome analysis to identify direct protein substrates of small-molecule degraders [ bioRxiv, 2024, 10.1101/2024.01.28.577572] | PubMed: none |
IMiDs Augment CD3-Bispecific Antibody-Induced CD8+ T-Cell Cytotoxicity and Expansion by Enhancing IL2 Production [ Mol Cancer Ther, 2023, 22(5):659-666] | PubMed: 36822576 |
IMiDs Augment CD3-Bispecific Antibody-Induced CD8+ T-Cell Cytotoxicity and Expansion by Enhancing IL2 Production [ Mol Cancer Ther, 2023, 22(5):659-666] | PubMed: 36822576 |
Lenalidomide bypasses CD28 co-stimulation to reinstate PD-1 immunotherapy by activating Notch signaling [ Cell Chem Biol, 2022, S2451-9456(22)00204-5] | PubMed: 35732177 |
Tyrphostin AG1024 Suppresses Coronaviral Replication by Downregulating JAK1 via an IR/IGF-1R Independent Proteolysis Mediated by Ndfip1/2_NEDD4-like E3 Ligase Itch [ Pharmaceuticals (Basel), 2022, 15(2)241] | PubMed: 35215353 |
Novel Peptide-drug Conjugate Melflufen Efficiently Eradicates Bortezomib-resistant Multiple Myeloma Cells Including Tumor-initiating Myeloma Progenitor Cells [ Hemasphere, 2021, 5(7):e602] | PubMed: 34136753 |
Evaluation of the Small-molecule BRD4 Degrader CFT-2718 in Small-cell Lung Cancer and Pancreatic Cancer Models [ Mol Cancer Ther, 2021, 10.1158/1535-7163.MCT-20-0831] | PubMed: 34045230 |
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。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。