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AZD 5153 Sale

目录号 : GC13014

A BRD4 inhibitor

AZD 5153 Chemical Structure

Cas No.:1869912-39-9

规格 价格 库存 购买数量
5mg
¥914.00
现货
10mg
¥1,785.00
现货
25mg
¥3,549.00
现货

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Sample solution is provided at 25 µL, 10mM.

产品文档

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产品描述

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 [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].

Clinical trial: no data available.

Reference:
[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.

Chemical Properties

Cas No. 1869912-39-9 SDF
化学名 (3R)-4-[2-[4-[1-(3-methoxy-1,2,4-triazolo[4,3-b]pyridazin-6-yl)-4-piperidinyl]phenoxy]ethyl]-1,3-dimethyl-2-piperazinone
Canonical SMILES COC1=NN=C2N1N=C(N3CCC(C4=CC=C(OCCN5[C@H](C)C(N(C)CC5)=O)C=C4)CC3)C=C2
分子式 C25H33N7O3 分子量 479.6
溶解度 ≤20mg/ml in ethanol;20mg/ml in DMSO;20mg/ml in dimethyl formamide 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
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1 mg 5 mg 10 mg
1 mM 2.0851 mL 10.4254 mL 20.8507 mL
5 mM 0.417 mL 2.0851 mL 4.1701 mL
10 mM 0.2085 mL 1.0425 mL 2.0851 mL
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