Powder: -20°C for 3 years | In solvent: -80°C for 1 year
BETd-246 is an inhibitor of second-generation and PROTAC-based BET bromodomain (BRD), show antitumor activity.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
5 mg | Inquiry | $ 539.00 | |
10 mg | Inquiry | $ 789.00 | |
25 mg | Inquiry | $ 1,610.00 | |
50 mg | Inquiry | $ 2,440.00 | |
100 mg | Inquiry | Inquiry | |
200 mg | Inquiry | Inquiry |
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) causes a dose-dependent depletion of BRD2, BRD3 and BRD4 in representative TNBC cell lines with 30-100 nM for 1 h or with 10-30 nM for 3 h incubation. BETd-246 (100 nM, 24/48 hours) displays strong growth inhibition and apoptosis induction activity in MDA-MB-468 cell lines. BETd-246 (100 nM, 24 hours) induces pronounced cell cycle arrest and apoptosis in TNBC cell lines[1]. BETd-246 induces a rapid and time-dependent downregulation of MCL1 protein in all the TNBC cell lines evaluated and it also induces much stronger apoptosis than BETi-211. |
In vivo | BETd-246 (5 mg/kg, IV, 3 times per week for 3 weeks) treatment effectively inhibits WHIM24 tumor growth, similar to the antitumor activity of BETi-211 with higher dosage and more frequently administration. BETd-246 has very limited drug exposure in the xenograft tumor tissue in MDA-M-231and MDA-MB-468 models[1]. The treatment of 10 mg/kg induces partial tumor regression during treatment without apparent toxicity. |
Molecular Weight | 946.02 |
Formula | C48H55N11O10 |
CAS No. | 2140289-17-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 200 mg/mL (211.41 mM), Sonication is recommended.
You can also refer to dose conversion for different animals. More
bottom
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
BETd-246 2140289-17-2 Others BETd246 BETd 246 inhibitor inhibit