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编 号：F747282
分子式：C22H26O6
分子量：386.44
分子式：C22H26O6
分子量：386.44
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CAS No: 181377-06-0
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生物活性：
Colletofragarone A2 can be be isolated from the fungus Colletotrichum?sp. (13S020). Colletofragarone A2 inhibits mutant p53 and HSP90 with anti-cancer activity. Colletofragarone A2 promotes degradation and aggregation of mutant p53 and suppressing tumor growth in vivo.
体内研究：
Colletofragarone A2 (0.35 mM, 100 μL; injected intratumorally and daily; 13 d) markedly decreases tumor cell growth in mouse infected with HuCCT1 (p53R175H) cells.Animal Model:Xenograft model with HuCCT1 (p53R175H) cells in mouse
Dosage:0.35 mM with 100 μL (DMSO solution)
Administration:Injected intratumorally; daily; 13 days; tested tumor growth at 1, 3, 5, 7, 9, 13 days
Result:Inhibited tumor growth without lowing body weight of mouse.
体外研究：
Mutant p53 loses original tumor suppressor function but acquires new abilities regarding oncogenic progression. Colletofragarone A2 (0.05-5 μM; 72 h) shows high selectivity and more cytotoxic activity on cells with p53R175H?structural mutants than with other p53 statuses such as a DNA-contact mutant, wild-type, and null cells. Colletofragarone A2 (2 μM; 8 h) decreases mutant p53 levels in SK-BR-3 (p53R175H) cells by promoting p53 degradation.Colletofragarone A2, combinded with 10 μM MG-132 (HY-13259), (2 or 4 μM; 4 h) induces the accumulation of the aggregated mutant p53.
Colletofragarone A2 can be be isolated from the fungus Colletotrichum?sp. (13S020). Colletofragarone A2 inhibits mutant p53 and HSP90 with anti-cancer activity. Colletofragarone A2 promotes degradation and aggregation of mutant p53 and suppressing tumor growth in vivo.
体内研究：
Colletofragarone A2 (0.35 mM, 100 μL; injected intratumorally and daily; 13 d) markedly decreases tumor cell growth in mouse infected with HuCCT1 (p53R175H) cells.Animal Model:Xenograft model with HuCCT1 (p53R175H) cells in mouse
Dosage:0.35 mM with 100 μL (DMSO solution)
Administration:Injected intratumorally; daily; 13 days; tested tumor growth at 1, 3, 5, 7, 9, 13 days
Result:Inhibited tumor growth without lowing body weight of mouse.
体外研究：
Mutant p53 loses original tumor suppressor function but acquires new abilities regarding oncogenic progression. Colletofragarone A2 (0.05-5 μM; 72 h) shows high selectivity and more cytotoxic activity on cells with p53R175H?structural mutants than with other p53 statuses such as a DNA-contact mutant, wild-type, and null cells. Colletofragarone A2 (2 μM; 8 h) decreases mutant p53 levels in SK-BR-3 (p53R175H) cells by promoting p53 degradation.Colletofragarone A2, combinded with 10 μM MG-132 (HY-13259), (2 or 4 μM; 4 h) induces the accumulation of the aggregated mutant p53.
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