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A-485
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
A-485图片
CAS NO:1889279-16-6
规格:98%
分子量:536.48
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
A-485是p300/CBP的强效选择性催化抑制剂,对p300和CBP的IC50值分别为9.8nM和2.6nM。
CAS:1889279-16-6
分子式:C25H24F4N4O5
分子量:536.48
纯度:98%
存储:Store at -20°C

Background:

A-485 is a potent and selective catalytic inhibitor of p300/CBP with IC50s of 9.8 nM and 2.6 nM for p300 and CBP, respectively.


A three-hour treatment of prostate adenocarcinoma PC-3 cells with A-485 results in a dose-dependent decrease in H3K27Ac, with a half maximal effective concentration (EC50) of 73 nM. Treatment with A-485 does not alter p300 or CBP protein levels. The broadest sensitivity is observed in haematological tumours, where A-485 exhibits potent activity in most multiple myeloma cell lines, and in a subset of acute myeloid leukaemia lines and non-Hodgkin’s lymphoma lines. A-485 induces a comparable decrease in H3K27Ac in all five prostate cancer cell lines. Treatment of the androgen-dependent LnCaP-FGC cell line with A-485 attenuates dihydrotestosterone (DHT) stimulated prostate-specific antigen (PSA) expression[1].


After tumours are established in SCID male mice, twice daily intraperitoneal injections of A-485 induce 54% tumour growth inhibition after 21 days of dosing (PMYC and the AR-dependent gene SLC45A3 at three hours post-dosing, and (for MYC) a decrease in the protein level, indicating that A-485 inhibits p300-mediated transcriptional activity in vivo. However, at 16 hours post-dosing on the seventh day, A-485 drug levels in the plasma and tumour are decreased as compare to 3 hours. A-485 induces a moderate 9% body weight loss, and the animals recover rapidly upon completion of the A-485 dosing regimen[1].


[1]. Lasko LM, et al. Discovery of a selective catalytic p300/CBP inhibitor that targets lineage-specific tumours. Nature. 2017 Oct 5;550(7674):128-132.