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
- Molecular Weight:
- 479.57
- MDL Number:
- MFCD30530420
- MOL File:
- 1869912-39-9.mol
| 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) |
| FDA UNII | C7C7U6YEAO |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|---|---|
| Signal word | Warning |
| Hazard statements | H315-H319-H335 |
| Precautionary statements | P261-P264-P271-P280-P302+P352-P304+P340-P305+P351+P338-P312-P332+P313 |
AZD5153 price More Price(8)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 20864 | AZD 5153 ≥95% | 1869912-39-9 | 1mg | $38 | 2024-03-01 | Buy |
| Cayman Chemical | 20864 | AZD 5153 ≥95% | 1869912-39-9 | 5mg | $176 | 2024-03-01 | Buy |
| Cayman Chemical | 20864 | AZD 5153 ≥95% | 1869912-39-9 | 10mg | $292 | 2024-03-01 | Buy |
| Cayman Chemical | 20864 | AZD 5153 ≥95% | 1869912-39-9 | 25mg | $593 | 2024-03-01 | Buy |
| ApexBio Technology | C3076 | AZD5153 | 1869912-39-9 | 25mg | $677 | 2021-12-16 | Buy |
AZD5153 Chemical Properties,Uses,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
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32480 | 60 |
| Career Henan Chemica Co | +86-0371-86658258 15093356674; | laboratory@coreychem.com | China | 30255 | 58 |
| HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6313 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10523 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
| Aladdin Scientific | +1-833-552-7181 | sales@aladdinsci.com | United States | 52927 | 58 |
| Amadis Chemical Company Limited | 571-89925085 | sales@amadischem.com | China | 131981 | 58 |
| ShangHai Caerulum Pharma Discovery Co., Ltd. | 18149758185 | sales-cpd@caerulumpharma.com | China | 3421 | 58 |
| Sichuan Wei Keqi Biological Technology Co., Ltd. | 028-81700200 18116577057 | 3003855609@qq.com | China | 7892 | 56 |
| Shanghai Lollane Biological Technology Co.,Ltd. | 021-52996696，15000506266 15000506266 | China | 4121 | 55 |