产品
编 号:F516188
分子式:C28H27NaO3
分子量:434.5
产品类型
结构图
CAS No: 911110-93-5
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产品详情
生物活性:
Adapalene (CD271) sodium salt, a third-generation synthetic retinoid, is widely used for the research of acne. Adapalene sodium salt is a potent RAR agonist, with AC50s of 2.3 nM, 9.3 nM, and 22 nM for RARβ, RARγ, RARα, respectively. Adapalene sodium salt also inhibits the enzymatic activity of GOT1 in a non-competitive manner. Adapalene sodium salt exhibits anti-tumor activity.
体内研究:
Adapalene sodium salt (15-100 mg/kg; p.o. daily for 21 days) inhibits the growth of DLD1 cell-derived xenograft tumors in BALB/C nude mice.Animal Model:Female BALB/C nude mice (15 g, 4-5 weeks) were injected with DLD1 cells
Dosage:15, 20, 65, 100 mg/kg
Administration:P.o. daily for 21 days
Result:Significantly reduced tumor weight and volume.
体外研究:
Adapalene sodium salt (1-200 μM; 24 h) inhibits the viability of ES-2, HOV-7, MCF-7, Hela, SW1990, HT1080, and MM-468 cells, with IC50s of 10.36 μM, 10.81 μM, 12.00 μM, 19.08 μM, 19.52 μM, 21.70 μM, and 31.47 μM, respectively.Adapalene sodium salt (10-40 μM; 24 h) induces ES-2 cells apoptosis and inhibits proliferation in vitro.Adapalene sodium salt (3-30 μM; 6-24 h) significantly increases the G1-phase population in LoVo or DLD1 cells.Adapalene sodium salt (1-200 μM) inhibits GOT1 activity, with an IC50?of 21.79?μM.Adapalene sodium salt (10-6-10-3 nM) inhibits the expression of plasma membrane-associated enzyme transglutaminase Type I, with an IC50 of 2.5 nM.