BETd-260 manufacturers
- BETd-260
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- $132.00 / 1mg
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2025-05-17
- CAS:2093388-62-4
- Min. Order:
- Purity: 96.76%
- Supply Ability: 10g
- BETd-260
-
- $132.00 / 1mg
-
2025-05-16
- CAS:2093388-62-4
- Min. Order:
- Purity: 96.76%
- Supply Ability: 10g
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| | BETd-260 Basic information |
| Product Name: | BETd-260 | | Synonyms: | BETd-260;ZBC260;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-[5-[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1-oxo-1H-isoindol-4-yl]pentyl]-6-methoxy-;BETd-260/ZBC260;4-[(3-cyclopropyl-1-ethyl-1H-pyrazol-5-yl)amino]-7-(3,5-dimethyl-1,2-oxazol-4-yl)-N-{5-[2-(2,6-dioxopiperidin-3-yl)-1-oxo-2,3-dihydro-1H-isoindol-4-yl]pentyl}-6-methoxy-9H-pyrimido[4,5-b]indole-2-carboxamide | | CAS: | 2093388-62-4 | | MF: | C43H46N10O6 | | MW: | 798.89 | | EINECS: | | | Product Categories: | | | Mol File: | 2093388-62-4.mol |  |
| | BETd-260 Chemical Properties |
| density | 1.52±0.1 g/cm3(Predicted) | | storage temp. | -80°C, protect from light, stored under nitrogen | | solubility | DMSO : 25 mg/mL (31.29 mM);Water : < 0.1 mg/mL (insoluble) | | pka | 10.73±0.40(Predicted) | | form | Solid | | color | Off-white to light yellow |
| | BETd-260 Usage And Synthesis |
| Description | BETd-260 is a PROTAC connected by ligands for Cereblon and BET. It potently suppresses cell viability and induces apoptosis in hepatocellular carcinomca (HCC) cells. | | Uses | BETd-260 (ZBC 260) is a PROTAC connected by ligands for Cereblon and BET, with as low as 30 pM against BRD4 protein in RS4;11 leukemia cell line[1]. BETd-260 potently suppresses cell viability and robustly induces apoptosis in hepatocellular carcinoma (HCC) cells[2]. | | in vivo | BETd-260 (5 mg/kg, i.v., every other day, thrice a week for 3 weeks) causes rapid tumor regression with a maximum of >90% regression in mice bearing RS4;11 xenograft tumors, and with no body weight loss or other signs of toxicity in mice. BETd-260 (5 mg/kg, i.v.) degrades the BRD2, BRD3, and BRD4 proteins for more than 24 h, with robust cleavage of PARP and caspase-3, and strong down-regulation of c-Myc protein in RS4;11 xenograft mice model[1]. | | IC 50 | BRD4: <30 pM (IC50); BRD2: 30-100 pM (IC50); BRD3: 30-100 pM (IC50) | | 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. DOI:10.1021/acs.jmedchem.6b01816
[2] Zhang H, et al. Targeting BET Proteins With a PROTAC Molecule Elicits Potent Anticancer Activity in HCC Cells. Front Oncol. 2020;9:1471. Published 2020 Jan 14. DOI:10.3389/fonc.2019.01471 |
| | BETd-260 Preparation Products And Raw materials |
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