AZD5153 is a potent, selective, bivalent and orally available BET/BRD4 bromodomain with IC50 of 5 nM.
AZD5153 simultaneously binds to two bromodomains in BRD4; exhibits antitumor activity in multiple xenograft models of acute myeloid leukemia, multiple myeloma, and diffuse large B cell lymphoma.
Physicochemical Properties
M.Wt
667.75404
Formula
C36H41N7O6
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
DMSO: ≥ 34 mg/mL
Chemical Name/SMILES
2-Naphthalenecarboxylic acid, 6-hydroxy-, compd. with (3R)-4-[2-[4-[1-(3-methoxy-1,2,4-triazolo[4,3-b]pyridazin-6-yl)-4-piperidinyl]phenoxy]ethyl]-1,3-dimethyl-2-piperazinone (1:1)
References
1. Bradbury RH, et al. J Med Chem. 2016 Sep 8;59(17):7801-17.
2. Rhyasen GW, et al. Mol Cancer Ther. 2016 Nov;15(11):2563-2574.
3. Collins TA, et al. CPT Pharmacometrics Syst Pharmacol. 2017 Jun;6(6):357-364.
