化合物1A-116 T14004

Product Introduction
Bioactivity


英文名: 1A-116

描述: 1A-116 是 Rac1的抑制剂，对几种类型的癌症具有抗肿瘤和抗转移作用，如乳腺癌。

体外活性: 1A-116 shows lesser effect on MCF7::pcDNA.3 cells than on MCF7::C1199 cells. 1A-116 treatment decreases phospho-PAK1 levels in a time-dependent manner. The presence of 1A-116 reverts the PAK1 phosphorylation induced by 4-hydroxytamoxifen (Tam). The presence of 1A-116 also effectively reverts Rac1-PAK1-mediated estrogen receptor (ER) phosphorylation at Ser305[1]. 1A-116 shows a significant increase in antiproliferative activity on F3II cells, showing an IC50 value of 4 μM. A-116 also dramatically impairs Rac1 activation at low micromolar range (1 μM)[2].

体内活性: 每日以3 mg/kg 的剂量对小鼠进行1A-116治疗，能够减少约60%的全身性转移性肺结节的形成。在这个高度侵袭性乳腺癌模型中，对直径超过1mm的大结节（macronodules）进行1A-116治疗，可获得显著的抗肿瘤活性。1A-116的治疗使得总肺重量与对照组相比有所降低，使得总体重量与Balb/c小鼠的平均肺重量相似[2]。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 100 mg/mL (325.40 mM)
H2O : < 0.1 mg/mL (insoluble)


关键字: TIAM1 | inhibit | 1A 116 | 1A-116 | Ras | Rho GTPases | EGF | Apoptosis | 1A116 | circadian rhythms | Inhibitor

相关产品: CCG-100602 | NSC 23766 trihydrochloride | CCG-1423 | YH-306 | Rhosin hydrochloride | AZA1 | Y16 | CCG-222740 | SKLB-163 | Y16 acetate(429653-73-6 free base)

相关库: Anti-Cancer Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Cytoskeletal Signaling Pathway Compound Library | Anti-Cancer Active Compound Library | Bioactive Compound Library

化合物1A-116 T14004信息由TargetMol中国为您提供，如您想了解更多关于化合物1A-116 T14004报价、型号、参数等信息，欢迎来电或留言咨询。

注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途