TX-1123可用作动物模型中癌症治疗的治疗剂。细胞可渗透的，可逆的且具有底物竞争性的亚芳基-环戊二烯酮衍生的酪氨酸抑制蛋白，可作为原癌基因酪氨酸蛋白激酶Src（c-Src，IC | 50 | = 2.2μM），真核延伸因子2激酶的激酶抑制剂（eEF2-K，IC | 50 | = 3.2μM）和蛋白激酶A（PKA，IC | 50 | = 9.6μM）。已显示TX-1123抑制EGFR-K和PKC，但仅在高得多的浓度下（IC | 50 | = 320μM）。|此外，已报道TX-1123在HepG2（EC）中 TX-1123 may be useful as a therapeutic agent for cancer treatment in animal models. A cell-permeable, reversible and substrate-competitive arylidene-cyclopentenedione derived tyrphostin that acts as a kinase inhibitor for proto-oncogene tyrosine-protein kinase Src (c-Src, IC|50|= 2.2 μM), eukaryotic elongation factor-2 kinase (eEF2-K, IC|50|= 3.2 μM), and protein kinase A (PKA, IC|50|= 9.6 μM). TX-1123 has been shown to inhibit EGFR-K and PKC, but only at much higher concentrations (IC|50|= 320 μM).|Additionally, TX-1123 has been reported to exhibit potent anti-tumor activity in HepG2(EC|50|= 3.66) and HCT116 (EC|50|= 39 μM) tumor cells, with greatly reduced mitochondrial- (≥1000-fold) and hepato-toxicity (≥50-fold) when compared with another tyrphostin, AG 17 .
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TX-1123
CAS number：157397-06-3 molecular formula：C20H24O3
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Specs
| Chinese alias | - | ||
| English alias | 2-((3,5-di-tert-Butyl-4-hydroxyphenyl)-methylene)-4-cyclopentene-1,3-dione | ||
| CAS number | 157397-06-3 | molecular formula | C20H24O3 |
| molecular weight | 312.4 g/mol | Exact mass | - |
| PSA | 54.400 Ų | logp | 5.100 |
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