PARP/PI3K-IN-1 (compound 15) 是一种有效的PARP/PI3K抑制剂，对 PARP-1，PARP-2，PI3Kα，PI3Kβ，PI3Kδ 和 PI3Kγ 的pIC50值分别为 8.22、8.44、8.25、6.54、8.13、6.08。PARP/PI3K-IN-1 是针对多种肿瘤疾病的高效抗癌化合物。
| 生物活性 | PARP/PI3K-IN-1 (compound 15) is a potentPARP/PI3Kinhibitor withpIC50values of 8.22, 8.44, 8.25, 6.54, 8.13, 6.08 for PARP-1, PARP-2,PI3Kα,PI3Kβ,PI3Kδ, andPI3Kγ, respectively. PARP/PI3K-IN-1 is a highly effective anticancer compound targeted against a wide range of oncologic diseases[1]. |
| IC50& Target[1] | PARP-1 8.22 (pIC50) | PARP-2 8.44 (pIC50) | PI3Kα 8.25 (pIC50) | PI3Kδ 8.13 (pIC50) | PI3Kγ 6.08 (pIC50) | PI3Kβ 6.54 (pIC50) |
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体外研究
(In Vitro) | PARP/PI3K-IN-1 (compound 15; 1 μM; 72 hours) leads to a significant increase in cell apoptosis[1].
PARP/PI3K-IN-1 (1 μM; 72 hours) reduces the autophosphorylation levels of AKT and S6 while increases the autophosphorylation level of ERK after treating cells, indicating that it can inhibit the PI3K pathway and activate the ERK pathway[1].
PARP/PI3K-IN-1 (1 μM) displays a strong capability to downregulate the expression of BRCA1/2 at the mRNA level in MDA-MB-468 cancer cells[1].
PARP/PI3K-IN-1 not only shows significant inhibitory activity against BRCA-deficient cells HCC1937 and HCT116, but also displays potent anti-proliferative activity against BRCA-proficient cells MDA-MB-231 and MDA-MB-468[1].
Apoptosis Analysis[1] | Cell Line: | MDA-MB-468 cancer cells | | Concentration: | 1 μM | | Incubation Time: | 72 hours | | Result: | Led to a significant increase in cell apoptosis. |
Western Blot Analysis[1] | Cell Line: | MDA-MB-468 cancer cells | | Concentration: | 1 μM | | Incubation Time: | 72 hours | | Result: | Reduced the autophosphorylation levels of AKT and S6 while increased the autophosphorylation level of ERK after treating cells. |
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体内研究
(In Vivo) | PARP/PI3K-IN-1 (i.p.; 50 mg/kg; twice daily (BID) for 34 consecutive days) significantly suppresses the tumor growth[1].
| Animal Model: | Six-week-old male BALB/c nude mice with MDA-MB-468 cells[1] | | Dosage: | 50 mg/kg | | Administration: | i.p.; twice daily (BID) for 34 consecutive days | | Result: | Significantly suppressed the tumor growth. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
