ONO-8430506CAS号: 1354805-08-5分子式: C27H28FN3O3分子量: 461.53描述纯度储存/保存方法可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)
产品描述 | |
描述 |
ONO-8430506 is an orally available, potent autotaxin (ATX)/ENPP2 inhibitor (IC90: 100 nM) that inhibits ATX activity in mouse plasma.
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纯度 |
97%
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储存/保存方法 |
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
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基本信息 | |
可溶性/溶解性 |
DMSO:90.0 mg/mL (195.0 mM)
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生物活性 | |
靶点 |
autotaxin (ATX)/ENPP2 inhibitor:100 nM
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In vitro(体外研究) |
The IC50 values of ONO-8430506 against the lysophospholipase D (LysoPLD) activity of recombinant human ATX/ENPP2 are 5.1 nM and 4.5 nM, determined using synthetic fluorescent substrate (FS-3) and a natural substrate (16:0-LPC) assay, respectively.[2]
ONO-8430506 exhibits effective inhibition of lysophosphatidic acid (LPA) formation, demonstrating IC50 values of approximately 10 nM with both recombinant and plasma-derived ATX/ENPP2 derived from diverse animal species.[2] |
In vivo(体内研究) |
ONO-8430506 (10 mg/kg/day; gavage; for 21 days). Tumor growth in ONO-8430506-treated mice caught up to the vehicle group by day 13; thereafter, primary tumor size was not significantly different from the vehicle-treated mice. It can slows initial tumor growth and limits lung metastasis. ONO-8430506 decreases the initial phase of breast tumor growth and subsequent lung metastases by ~60% in a syngeneic orthotopic mouse model.[1]
ONO-8430506 (oral; 30 mg/kg) demonstrates good pharmacokinetics and persistently inhibits plasma lysophosphatidic acid formation in rats.[2] ONO-8430506 (30 or 100 mg/kg) enhances the antitumor effect of Paclitaxel in a breast cancer model.[3] ONO-8430506 exhibits moderate oral bioavailability (rat 51.6%, dog 71.1%, and monkey 30.8%) and C max (rat 261, dog 1670, and monkey 63 ng/mL) following oral administration (rat 1, dog 1, and monkey 1 mg/kg).[3] |