ChemicalBook > CAS DataBase List > AZD5153

AZD5153

Product Name
AZD5153
CAS No.
1869912-39-9
Chemical 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)-
CBNumber
CB63169779
Molecular Formula
C25H33N7O3
Formula Weight
479.57
MOL File
1869912-39-9.mol
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AZD5153 Property

Density 
1.34±0.1 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
≤20mg/ml in ethanol;20mg/ml in DMSO;20mg/ml in dimethyl formamide
form 
crystalline solid
pka
7.57±0.40(Predicted)
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P312Call a POISON CENTER or doctor/physician if you feel unwell.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

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N-Bromosuccinimide Price

Cayman Chemical
Product number
20864
Product name
AZD 5153
Purity
≥95%
Packaging
1mg
Price
$38
Updated
2024/03/01
Cayman Chemical
Product number
20864
Product name
AZD 5153
Purity
≥95%
Packaging
5mg
Price
$176
Updated
2024/03/01
Cayman Chemical
Product number
20864
Product name
AZD 5153
Purity
≥95%
Packaging
10mg
Price
$292
Updated
2024/03/01
Cayman Chemical
Product number
20864
Product name
AZD 5153
Purity
≥95%
Packaging
25mg
Price
$593
Updated
2024/03/01
ApexBio Technology
Product number
C3076
Product name
AZD5153
Packaging
25mg
Price
$677
Updated
2021/12/16
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AZD5153 Chemical Properties,Usage,Production

Description

AZD 5153 an orally available, bivalent inhibitor of the bromodomain and extraterminal (BET) protein BRD4 (IC50 = 5 nM). It can simultaneously bind two bromodomains in BRD4, which has been shown to increase antitumor activity in multiple xenograft models of acute myeloid leukemia, multiple myeloma, and diffuse large B cell lymphoma.

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

IC 50

5 nm

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.

AZD5153 Preparation Products And Raw materials

Raw materials

Preparation Products

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1869912-39-9, AZD5153Related Search:


  • CPD1544
  • AZD5153; AZD-5153; AZD 5153
  • CS-2562
  • 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)-
  • 1869912-39-9
  • C25H33N7O3