CAS NO: | 1889279-16-6 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
1mg | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
生物活性 | A-485 is a potent and selective catalytic inhibitor ofp300/CBPwithIC50s of 9.8 nM and 2.6 nM forp300andCBPhistone acetyltransferase(HAT), respectively[1]. | ||||||||||||||||
IC50& Target | IC50: 9.8 nM (p300), 2.6 nM (CBP)[1] | ||||||||||||||||
体外研究 (In Vitro) | 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[1]. | ||||||||||||||||
体内研究 (In Vivo) | 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 (P<0.005 as compare to vehicle control). In addition, in tumour-bearing animals, dosing with A-485 for seven days induces a decrease in the mRNA levels ofMYCand the AR-dependent geneSLC45A3at three hours post-dosing, and (for MYC) a decrease in the protein level, indicating that A-485 inhibits p300-mediated transcriptional activityin 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]. | ||||||||||||||||
分子量 | 536.48 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C25H24F4N4O5 | ||||||||||||||||
CAS 号 | 1889279-16-6 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 125 mg/mL(233.00 mM;Need ultrasonic) 配制储备液
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