Chemical Structure : BD-9136
CAS No.:
3037514-38-5
BD-9136
(BD9136)
Catalog No.: PC-24551Not For Human Use, Lab Use Only.
BD-9136 is a potent, highly selective PROTAC degrader of BRD4 with DC50 of 1.2 nM (MV-4-11 cell, 4 h), Dmax=99%, displays >1000-fold selective over BRD2 and BRD3 proteins.
Bulk size, bulk discount!
Welcome credit card payment!
E-mail: sales@probechem.com
Tech Support: tech@probechem.com
Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
BD-9136 is a potent, highly selective PROTAC degrader of BRD4 with DC50 of 1.2 nM (MV-4-11 cell, 4 h), Dmax=99%, displays >1000-fold selective over BRD2 and BRD3 proteins.
BD-9136 is very potent and effective in inducing BRD4 degradation and achieves DC50 values of 0.1-4.7 nM and Dmax of >90% in 8 cancer cell lines.
BD-9136 potently inhibits cell growth inhibition in leukemia and breast cancer cell lines with IC50 of 5.1-80.9 nM.
BD-9136 significantly reduces only the level of BRD4 protein in the MDA-MB-231 cell line and does not significantly reduce any of the other >5,700 proteins, including BRD2 and BRD3 proteins.
BD-9136 effectively reduces the level of BRD4 protein in both the MV4;11 and MDA-MB-231 xenograft tumor tissues.
BD-9136 effectively inhibits tumor growth without adverse effects on mice and is more efficacious than the corresponding pan BET inhibitor.
Physicochemical Properties
|
M.Wt
|
824.96
|
|
Formula
|
C44H44N10O5S
|
|
Appearance
|
Solid
|
|
CAS No.
|
|
|
Storage
|
- Solide Powder
-
-20°C 12 Months; 4°C 6 Months
|
- In Solvent
-
-80°C 6 Months; -20°C 6 Months
|
|
Shipping
|
|
|
Solubility
|
10 mM in DMSO
|
|
Chemical Name/SMILES
|
1H-Isoindole-1,3(2H)-dione, 2-(2,6-dioxo-3-piperidinyl)-4-[3-[4-[2-[9-methyl-3-(phenylmethyl)-4H,6H-thieno[2,3-e][1,2,4]triazolo[3,4-c][1,4]oxazepin-2-yl]ethynyl]-1H-pyrazol-1-yl]-3-[2-(4-methyl-1-piperazinyl)ethyl]-1-azetidinyl]-
|
References
1. Hu J, et al. J Med Chem. 2023 Jun 22;66(12):8222-8237.
Contact Us
sales@probechem.com
