產(chǎn)品目錄

規(guī)格	5mg 25mg
CAS	1802088-50-1
別名	N/A
化學(xué)名	8-((4-(cyclopropanecarbonyl)piperazin-1-yl)methyl)-7-isopentyl-1,3-dimethyl-1H-purine-2,6(3H,7H)-dione
分子式	C21H32N6O3
分子量	416.52
溶解度	≥ 20.85mg/mL in DMSO with gentle warming
儲存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

NCT-501 is a potent and selective theophylline-based inhibitor of aldehyde dehydrogenase 1A1 (ALDH1A1).Aldehyde dehydrogenases (ALDHs) metabolize reactive aldehydes and play important physiological and toxicological functions in metabolic disorders and cancers. ALDH1A1can be used as the marker of malignant prostate stem cells and predictor of prostate cancer patients' outcome. Over-expression of ALDH is associated with some types of cancers. Selective inhibitors targeted ALDH isozymes could preventspheroids formation in vitro and the size of xenograft tumors formed in vivo.

For more than 450 human kinases, NCT-501 treatment at 10 μM inhibited ≥55% activity of these kinases. NCT-501 reversibly inhibited ALDH1A1.The plasma exposure for intraperitoneal administration (ip) at 30 mg/kg showed better than the oral administration (p.o) at 30 mg/kg. The values of AUC 24h were 5670 h·ng/mL and 484 h·ng/mL along with 100% and 29% bioavailability, respectively. The t1/2 was shorter than 1h. The clearance level was 98 mL/min/kg. These results together indicated that NCT-501 was well absorbed and distributed but rapidly metabolized or excreted. In vitro stability of NCT-501in CD1 mouse plasma was more than 60 min

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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