产品
编 号:F170074
分子式:C16H14N2O2
分子量:266.29
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规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
336
In-stock
5mg
800
In-stock
10mg
1360
In-stock
25mg
2491
In-stock
50mg
3464
In-stock
100mg
4960
In-stock
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生物活性:
Tyrphostin AG1296 is a potent and selective inhibitor of platelet-derived growth factor receptor (PDGFR), with an IC50 of 0.8 μM. Tyrphostin AG1296 inhibits signaling of human PDGF α- and β-receptors as well as of the related stem cell factor receptor (c-Kit). Tyrphostin AG1296 is also a potent inhibitor of FLT3, with an IC50 in the micromolar range.

体内研究:
Tyrphostin AG1296 (40 和 80 mg/kg;每天腹膜内注射,持续两周) 在体内抑制 A375R 肿瘤生长。Tyrphostin AG1296 (2 mg/kg;每隔一天腹膜内注射,持续 3 周) 通过抑制炎症反应、降低基质金属蛋白酶的表达、促进巨噬细胞从促炎表型向抗炎表型转变,从而抑制动脉粥样硬化斑块进展,增强斑块稳定性。Animal Model:Nud/nud mice are injected with A375R cells
Dosage:40, 80 mg/kg
Administration:I.p. daily for two weeks
Result:Led to an intermediate level of tumor growth suppression at dose of 40 mg/kg, and significant inhibition of A375R tumor growth at dose of 80 mg/kg.Well tolerated by healthy mice without significant signs of overt toxicity or weight loss.

体外研究:
Tyrphostin AG1296 (0.625 -20 μM;72 h) 抑制 PLX4032 耐药黑色素瘤细胞的活力。 Tyrphostin AG1296 (2.5 -20 μM;48 h) 诱导 A375R 细胞凋亡。 Tyrphostin AG1296 (5 和 20 μM;2 小时) 抑制 A375R 细胞中的 PDGFR 磷酸化。 Tyrphostin AG1296 (0.0625-1 μM;8 h) 抑制 A375R 细胞的迁移。
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