Synonym
dBET57; dBET-57; dBET 57;
IUPAC/Chemical Name
2-((S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-N-(2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)ethyl)acetamide
InChi Key
CZRLOIDJCMKJHE-UXMRNZNESA-N
InChi Code
InChI=1S/C34H31ClN8O5S/c1-16-17(2)49-34-27(16)29(19-7-9-20(35)10-8-19)38-23(30-41-40-18(3)42(30)34)15-26(45)37-14-13-36-22-6-4-5-21-28(22)33(48)43(32(21)47)24-11-12-25(44)39-31(24)46/h4-10,23-24,36H,11-15H2,1-3H3,(H,37,45)(H,39,44,46)/t23-,24?/m0/s1
SMILES Code
O=C(NCCNC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)C[C@H]4C5=NN=C(C)N5C6=C(C(C)=C(C)S6)C(C7=CC=C(Cl)C=C7)=N4
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Preparing Stock Solutions
The following data is based on the
product
molecular weight
699.18
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
1: Jia SQ, Zhuo R, Zhang ZM, Yang Y, Tao YF, Wang JW, Li XL, Xie Y, Li G, Wu D,
Chen YL, Yu JJ, Feng CX, Li ZH, Zhou RF, Yang RD, Yang PC, Zhou B, Wan XM, Wu
YM, Jiao WY, Zhou NN, Fang F, Pan J. The BRD4 Inhibitor dBET57 Exerts Anticancer
Effects by Targeting Superenhancer-Related Genes in Neuroblastoma. J Immunol
Res. 2022 Nov 16;2022:7945884. doi: 10.1155/2022/7945884. PMID: 36438198; PMCID:
PMC9691391.
2: Zhao LP, Zheng RR, Rao XN, Huang CY, Zhou HY, Yu XY, Jiang XY, Li SY.
Chemotherapy-Enabled Colorectal Cancer Immunotherapy of Self-Delivery Nano-
PROTACs by Inhibiting Tumor Glycolysis and Avoiding Adaptive Immune Resistance.
Adv Sci (Weinh). 2024 Apr;11(15):e2309204. doi: 10.1002/advs.202309204. Epub
2024 Jan 18. PMID: 38239040; PMCID: PMC11022706.
3: Lang C, Stickler S, Rath B, Teufelsbauer M, Weigl L, Hohenegger M, Hamilton
G. BRD4-targeting PROTACs Synergize With Chemotherapeutics Against Osteosarcoma
Cell Lines. Anticancer Res. 2024 Mar;44(3):971-980. doi:
10.21873/anticanres.16892. PMID: 38423674.
4: Zhao LP, Rao XN, Zheng RR, Huang CY, Kong RJ, Cheng H, Li B, Li SY. Carrier-
Free Nano-PROTACs to Amplify Photodynamic Therapy Induced DNA Damage through
BRD4 Degradation. Nano Lett. 2023 Jul 12;23(13):6193-6201. doi:
10.1021/acs.nanolett.3c01812. Epub 2023 Jun 30. PMID: 37387510.
