S34302 |
PARP/PI3K-IN-1 |
源葉(MedMol) | 98% |
- 產(chǎn)品描述:
PARP/PI3K-IN-1 (compound 15) 是一種有效的 PARP/PI3K 抑制劑,對 PARP-1,PARP-2,PI3Kα,PI3Kβ,PI3Kδ 和 PI3Kγ 的 pIC50 值分別為 8.22、8.44、8.25、6.54、8.13、6.08。PARP/PI3K-IN-1 是針對多種腫瘤疾病的高效抗癌化合物。
- 靶點: PI3K
- 體外研究:
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.
- 體內(nèi)研究:
PARP/PI3K-IN-1 (i.p.; 50 mg/kg; twice daily (BID) for 34 consecutive days) significantly suppresses the tumor growth.
- 參考文獻:
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).
- 保存條件: -20℃
- 配置溶液濃度參考:
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
- 注意:部分產(chǎn)品我司僅能提供部分信息,我司不保證所提供信息的權(quán)威性,僅供客戶參考交流研究之用。
輸入產(chǎn)品批號:
本計算器可幫助您計算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關(guān)系,公式為:
質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)