S34302 |
PARP/PI3K-IN-1 |
源叶(MedMol) | 98% |
- 产品描述:
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。
- 靶点: PI3K
- 体外研究:
PARP/PI3K-IN-1 (compound 15; 1 μM; 72 hours) leads to a significant increase in cell apoptosis.
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.
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.
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.
- 体内研究:
PARP/PI3K-IN-1 (i.p.; 50 mg/kg; twice daily (BID) for 34 consecutive days) significantly suppresses the tumor growth.
- 参考文献:
1: Wang, J., Li, H., He, G., et al. Discovery of novel dual poly(ADP-ribose)polymerase (PARP) and phosphoinositide 3-kinase (PI3K) inhibitors as a promising strategy for cancer therapy. J. Med. Chem. 63(1), 122-139 (2019).
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 1.514 ml 7.569 ml 15.137 ml 5 mM 0.303 ml 1.514 ml 3.027 ml 10 mM 0.151 ml 0.757 ml 1.514 ml 50 mM 0.03 ml 0.151 ml 0.303 ml
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)