AG 957，金刚烷酯是酪蛋白 AG 957的亲脂性，金刚烷酸酯形式，具有抗增殖特性。已证明该产品具有选择性，比bcr / abl激酶抑制剂AG 957的效力高约3-4倍。AG957，金刚烷酯下调p210bcr / abl自身激酶活性（IC 50 = 14 µM）。通过诱导细胞凋亡，选择性阻断CML（慢性粒细胞性白血病）祖细胞中粒细胞集落的形成，并抑制K562细胞的增殖（IC 50 = 9.8 µM）。据报道，AG 957，金刚烷酯在STI571耐药和p53无效的人类白血病细胞系（IC 50〜0.1-0. AG 957, Adamantyl Ester is a lipophilic, adamantyl ester form of tyrphostin AG 957 that displays anti-proliferative properties. The product has been shown to be selective and is ~3-4 fold more potent than the bcr/abl kinase inhibitor AG 957. AG 957, Adamantyl Ester Downregulates p210bcr/abl autokinase activity (IC|50|= 14 µM). Selectively blocks granulocyte colony formation in CML (chronic myelogenous leukemia) progenitors and inhibits proliferation of K562 cells (IC|50|= 9.8 µM) by inducing apoptosis. AG 957, Adamantyl Ester is reported to retain activity in STI571-resistant and p53-null human leukemia cell lines (IC|50|~0.1-0.25 µM). AG 957, Adamantyl Esteris an ~3-4 fold more potent derivative of AG 957
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AG 957, Adamantyl Ester
CAS number：241127-58-2 molecular formula：C24H27NO4
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compound introduction
Specs
| Chinese alias | - | ||
| English alias | NSC 680410 | Adaphostin | 4-[[(2,5-Dihydroxyphenyl)methyl]amino]benzoic acid tricyclo[3.3.1.13,7]dec-1-yl ester | ||
| CAS number | 241127-58-2 | molecular formula | C24H27NO4 |
| molecular weight | 393.48 g/mol | Exact mass | ≥98% |
| PSA | 78.800 Ų | logp | 5.200 |
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