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| | PROTAC 11 Basic information |
| Product Name: | PROTAC 11 | | Synonyms: | PROTAC 11;PROTAC BET Degrader-1;9H-Pyrimido[4,5-b]indole-2-carboxamide, 4-[(3-cyclopropyl-1-ethyl-1H-pyrazol-5-yl)amino]-7-(3,5-dimethyl-4-isoxazolyl)-N-[4-[[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]acetyl]amino]butyl]-6-methoxy-;N-[4-({4-[(3-cyclopropyl-1-ethyl-1H-pyrazol-5-yl)amino]-7-(3,5-dimethyl-1,2-oxazol-4-yl)-6-methoxy-9H-pyrimido[4,5-b]indol-2-yl}formamido)butyl]-2-{[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl]oxy}acetamide;4-[(3-Cyclopropyl-1-ethyl-1H-pyrazol-5-yl)amino]-7-(3,5-dimethyl-4-isoxazolyl)-N-[4-[[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]acetyl]amino]butyl]-6-methoxy-9H-pyrimido[4,5-b]indole-2-carboxamide | | CAS: | 2093386-22-0 | | MF: | C44H45N11O9 | | MW: | 871.9 | | EINECS: | | | Product Categories: | | | Mol File: | 2093386-22-0.mol |  |
| | PROTAC 11 Chemical Properties |
| density | 1.59±0.1 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | DMSO : ≥ 50 mg/mL (57.35 mM) | | pka | 10.68±0.40(Predicted) | | form | Solid | | color | Light yellow to yellow |
| | PROTAC 11 Usage And Synthesis |
| Description | PROTAC BET Degrader-1 is a potent BET degrader based on PROTAC, decreasing BRD2, BRD3, and BRD4 protein levels at low concentration. PROTAC BET Degrader-1 (Compound 9) is a potent BET degrader based on PROTAC, decreases the level of BRD2, BRD3, and BRD4 proteins in RS4;11 cells at 3-10 nM, and inhibits the growth of this cell line with an IC50 of 4.3 nM, and 45.5 nM for MOLM-13 cells[1]. | | Uses | PROTAC BET Degrader-1 is a PROTAC connected by ligands for Cereblon and BET, decreasing BRD2, BRD3, and BRD4 protein levels at low concentration. | | References | [1]. Zhou B, et al. Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression. J Med Chem. 2018 Jan 25;61(2):462-481. |
| | PROTAC 11 Preparation Products And Raw materials |
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