dBET57
CAS No. : 1883863-52-2
| Size | Price | Stock |
|---|---|---|
| 5mg | $120 | In-stock |
| 10mg | $195 | In-stock |
| 25mg | $350 | In-stock |
| 50mg | $570 | In-stock |
| 100mg | $795 | In-stock |
| 200 mg | Get quote | |
| 500 mg | Get quote | |
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| Cat. No. : | HY-123844 |
| M.Wt: | 699.18 |
| Formula: | C34H31ClN8O5S |
| Purity: | >98 % |
| Solubility: | DMSO : 250 mg/mL (ultrasonic) |
dBET57 is an effective and selective BRD4BD1 degrader based on PROTAC technology, with the ability to induce cell apoptosis and anti-tumor activity. dBET57 mediates the recruitment of the E3 ubiquitin ligase CRL4Cereblon, showing a DC50/5h value of 500 nM for BRD4BD1[1][2].
IC50 & Target:DC50/5h: 500 nM (BRD4BD1)[1]
In Vitro:dBET57 (0-10000 nM, 72 h) inhibits the proliferation of NB cells, with the IC50 values for SK-N-BE(2), IMR-32, SH-SY5Y, HT22, HPAEC, 293T, HCAEC being 643.4, 299, 414, 2151, 2321, 4840 and 3939 nM[1].
dBET57 (0-1200 nM, 48 h) induces apoptosis in NB cells, and increases the proportion of cells in the G1 phase[1].
dBET57 (0-1200 nM, 0-48 h) reduces the migration and adhesion capabilities of NB cells[1].
In Vivo:dBET57 (7.5 mg/kg, intraperitoneal injection, once daily, 2 weeks) has antitumor activity in the SK-NBE(2) xenograft mouse model[1].
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