Target: BRD4 IC50: 5 nM AZD5153 is a potent, selective, and orally available inhibitor of the bromodomain and extraterminal (BET) protein BRD4, with the IC50 value of 5 nM. AZD5153 could simultaneously ligate two bromodomains in BRD4, and exert antitumor activity in multiple xenograft tumor models . In Vitro: A quantitative immuno-fluorescent assay in U2OS cells revealed that AZD5153 could significantly disrupt BRD4 foci, with the IC50 value of 1.7 nM. Besides, AZD5153 could inhibit the proliferation of AML, MM, and DLBCL cell lines, with the majority of cell lines having a GI50 value < 25 nM. Furthermore, 200 nM AZD5153 could significantly decrease the level of mTOR pathway associated proteins in sensitive hematologic cancer cell lines (MOLP8, MV-4-11, OCILY19) . In Vivo: In AML, MM, and DLBCL xenografted tumor mouse models, oral administration of AZD5153 at the dose of 1, 2.5, and 5mg/kg could inhibit tumor growth in a dose dependent manner . Clinical trial: no data available.

Product information

CAS Number: 1869912-39-9

Molecular Weight: 479.57

Formula: C25H33N7O3

Chemical Name: (3R)-4-{2-[4-(1-{3-methoxy-[1,2,4]triazolo[4,3-b]pyridazin-6-yl}piperidin-4-yl)phenoxy]ethyl}-1,3-dimethylpiperazin-2-one

Smiles: CN1CCN(CCOC2C=CC(=CC=2)C2CCN(CC2)C2C=CC3=NN=C(OC)N3N=2)[C@H](C)C1=O

InChiKey: RSMYFSPOTCDHHJ-GOSISDBHSA-N

InChi: InChI=1S/C25H33N7O3/c1-18-24(33)29(2)14-15-30(18)16-17-35-21-6-4-19(5-7-21)20-10-12-31(13-11-20)23-9-8-22-26-27-25(34-3)32(22)28-23/h4-9,18,20H,10-17H2,1-3H3/t18-/m1/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

Products are for research use only. Not for human use.