1869912-39-9

Basic information

• Product Name: AZD5153
• Synonyms: CPD1544;CS-2562;AZD5153; AZD-5153; AZD 5153;2-Piperazinone, 4-[2-[4-[1-(3-methoxy-1,2,4-triazolo[4,3-b]pyridazin-6-yl)-4-piperidinyl]phenoxy]ethyl]-1,3-dimethyl-, (3R)-
• CAS NO: 1869912-39-9
• Molecular Formula: C25H33N7O3
• Molecular Weight: 479.57462
• Mol File: 1869912-39-9.mol

Chemical Properties

• Appearance: /
• Solubility: ≤20mg/ml in ethanol;20mg/ml in DMSO;20mg/ml in dimethyl formamide
• CAS DataBase Reference: AZD5153(CAS DataBase Reference)
• NIST Chemistry Reference: AZD5153(1869912-39-9)
• EPA Substance Registry System: AZD5153(1869912-39-9)

Safety Data

• Hazardous Substances Data: 1869912-39-9(Hazardous Substances Data)

Usage

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) [1].

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 [1].

target

brd4

references

[1] rhyasen g w, hattersley m m, yao y, et al. azd5153: a novel bivalent bet bromodomain inhibitor highly active against hematologic malignancies[j]. molecular cancer therapeutics, 2016, 15(11): 2563-2574.

Upstream product

• 286961-24-8 benzyl 1,2,3,6-tetrahydro-4-(trifluoromethylsulphonyloxy)-pyridine-1-carboxylate 
• 1166820-03-6 benzyl 4-(4-hydroxyphenyl)-5,6-dihydropyridine-1(2H)-carboxylate 
• 62614-84-0 4-(4-hydroxyphenyl)-1,2,3,6-tetrahydropiperidine 
• 1869912-48-0 4-(piperidine-4-yl)phenol hydrobromide 
• 19099-93-5 benzyl 4-oxo-1-piperidinecarboxylate 
• 149377-19-5 4-(4-hydroxy-phenyl)-piperidine-1-carboxylic acid tert-butyl ester 

Relevant articles and documents

Optimization of a Series of Bivalent Triazolopyridazine Based Bromodomain and Extraterminal Inhibitors: The Discovery of (3R)-4-[2-[4-[1-(3-Methoxy-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)-4-piperidyl]phenoxy]ethyl]-1,3-dimethyl-piperazin-2-one (AZD5153)

Here we report the discovery and optimization of a series of bivalent bromodomain and extraterminal inhibitors. Starting with the observation of BRD4 activity of compounds from a previous program, the compounds were optimized for BRD4 potency and physical

[1,2,4]TRIAZOLO[4,3-B]PYRIDAZINES FOR USE IN THE TREATMENT OF PROLIFERATIVE DISEASES

The invention concerns compounds of Formula (I) (Formula (I)) or pharmaceutically-acceptable salts thereof, wherein R1, R2 and n have any of the meanings defined herein before in the description; processes for their preparation, pharmaceutical compositions containing them and their use as anti-proliferative and/or cell-killing agents.