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BETd-246
BETd-246 is an inhibitor of second-generation and PROTAC-based BET bromodomain (BRD), show antitumor activity.
Catalog No. T14549Cas No. 2140289-17-2
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BETd-246
Catalog No. T14549Cas No. 2140289-17-2
BETd-246 is an inhibitor of second-generation and PROTAC-based BET bromodomain (BRD), show antitumor activity.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose. | Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 5 mg | $539 | Backorder | |
| 10 mg | $789 | Backorder | |
| 25 mg | $1,610 | Backorder | |
| 50 mg | $2,440 | Backorder | |
| 100 mg | Inquiry | Backorder | |
| 200 mg | Inquiry | Backorder |
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | BETd-246 is an inhibitor of second-generation and PROTAC-based BET bromodomain (BRD), show antitumor activity. |
| In vitro | BETd-246 treatment (0-100 nM, 1-3 h) leads to a dose-dependent reduction of BRD2, BRD3, and BRD4 in TNBC cell lines, with optimal effects observed at 30-100 nM for 1 hour or 10-30 nM for 3 hours. BETd-246 (100 nM, 24/48 hours) significantly inhibits growth and induces apoptosis in MDA-MB-468 cell lines. Additionally, BETd-246 (100 nM, 24 hours) causes marked cell cycle arrest and apoptosis in TNBC cell lines[1]. It induces rapid, time-dependent downregulation of MCL1 protein in all evaluated TNBC cell lines and exhibits stronger apoptosis induction than BETi-211. |
| In vivo | BETd-246 (5 mg/kg, IV, 3 times per week for 3 weeks) effectively inhibits WHIM24 tumor growth, similar to the antitumor activity of BETi-211 at a higher dose with more frequent administration. BETd-246 exhibits limited drug exposure in xenograft tumor tissue in MDA-M-231 and MDA-MB-468 models[1]. A dose of 10 mg/kg induces partial tumor regression during treatment without apparent toxicity. |
| Molecular Weight | 946.02 |
| Formula | C48H55N11O10 |
| Cas No. | 2140289-17-2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 200 mg/mL (211.41 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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