105798-74-1
105798-74-1 結(jié)構(gòu)式
基本信息
中文別名
克力托辛 英文別名
clitocineN-(6-Amino-5-nitro-4-pyrimidinyl)-β-D-ribofuranosylamine
b-D-RibofuranosylaMine, N-(6-aMino-5-nitro-4-pyriMidinyl)-
N-(6-Amino-5-nitro-4-pyrimidinyl)-beta-D-ribofuranosylamine
β-D-Ribofuranosylamine, N-(6-amino-5-nitro-4- pyrimidinyl)-
常見問題列表
生物活性
Clitocine 是一種來源于蘑菇的腺苷核苷類似物，是一種有效的通讀劑 (readthrough)。Clitocine 作為一種無義突變 (nonsense mutations) 的抑制劑，可誘導(dǎo)攜帶 p53 無義突變等位基因的細(xì)胞產(chǎn)生 p53 蛋白。Clitocine 可通過靶向 Mcl-1 誘導(dǎo)多藥耐藥腫瘤細(xì)胞凋亡。具有抗癌活性。體外研究
Clitocine incorporation into mRNA is required for premature stop codon readthrough activity, and the presence of clitocine at the third position of a premature stop codon is sufficient to promote robust readthrough.
Clitocine (0-0.8 μM; 24 hours) enhances TRAIL-lethality in in LS411N and SW620 cells. Clitocine (0.2μM; 36 hours) significantly potentiates TRAIL-mediated apoptosis.
體內(nèi)研究
Citocine (0.3-3 mg/kg; s.c.; five times per week)-induced p53 inhibits CAOV-33 p53-UAA136 tumor growth in a xenograft model.
| Animal Model: | nu/nu mice (CAOV-3p53-UAA136 xenograft tumors) |
| Dosage: | 0.3, 3 mg/kg (or 20 mg/kg once per week) |
| Administration: | S.c.; five times per week |
| Result: | CAOV-33 p53-UAA136 tumor growth was inhibited. |