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Inavolisib
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Inavolisib
CAS No. : 2060571-02-8
MCE 站:Inavolisib
产品活性:GDC-0077 (RG6114) 是一种有效的,口服的选择性 PI3Kα 抑制剂 (IC50=0.038 nM)。GDC-0077 (RG6114) 通过与 PI3K 的 ATP 结合位点结合而发挥其活性,从而抑制了 PIP2 到 PIP3 的磷酸化。与野生型 PI3Kα 相比,GDC-0077 (RG6114) 对突变体的选择性更高。
研究领域:PI3K/Akt/mTOR | Apoptosis
In Vitro: GDC-0077 (RG6114) is >300-fold more selective for PI3Kα over the other class I PI3K isoforms (β, δ, and γ) and >2000-fold more selective over PIK family members. GDC-0077 selectively degrades mutant PI3Kα in a proteasome-dependent fashion resulting in reduction of PI3K pathway activity biomarkers such as pAKT and pPRAS40, inhibition of cell proliferation, and increased apoptosis in human PIK3CA-mutant breast cancer cell lines to a greater extent when compared to PIK3CA wild-type cells.
In Vivo: GDC-0077 (p.o.) results in tumor regressions, induction of apoptosis, and a reduction of pAKT, pPRAS40, and pS6RP in a dose-dependent fashion in patient-derived PIK3CA-mutant breast cancer xenograft models.
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