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
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)
- color
- Light yellow to light brown
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.
N-Bromosuccinimide Price
- Product number
- 20864
- Product name
- AZD 5153
- Purity
- ≥95%
- Packaging
- 1mg
- Price
- $38
- Updated
- 2024/03/01
- Product number
- 20864
- Product name
- AZD 5153
- Purity
- ≥95%
- Packaging
- 5mg
- Price
- $176
- Updated
- 2024/03/01
- Product number
- 20864
- Product name
- AZD 5153
- Purity
- ≥95%
- Packaging
- 10mg
- Price
- $292
- Updated
- 2024/03/01
- Product number
- 20864
- Product name
- AZD 5153
- Purity
- ≥95%
- Packaging
- 25mg
- Price
- $593
- Updated
- 2024/03/01
- Product number
- C3076
- Product name
- AZD5153
- Packaging
- 25mg
- Price
- $677
- Updated
- 2021/12/16
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.
Uses
AZD5153 (Compound 13) is a trivalent triazolpyrazine bromide domain (BRD), bromodomain and extraterminal (BET) inhibitor. AZD5153 has down-regulated c-Myc gene and tumor growth inhibition activity. AZD5153 can be used in the study of BET small molecule inhibitors [1].
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.
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