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Risovalisib

產(chǎn)品活性：Risovalisib (CYH33) 是一種具有口服活性的，高選擇性 PI3Kα 抑制劑，對(duì) α/β/δ/γ 亞型的 IC₅₀ 分別為 5.9 nM/598 nM/78.7 nM/225 nM。Risovalisib 抑制 Akt 和 ERK 的磷酸化，并顯著誘導(dǎo)乳腺癌和非小細(xì)胞肺癌 (NSCLC) 細(xì)胞 G1 期阻滯。Risovalisib 具有有效的抗實(shí)體瘤的活性。

研究領(lǐng)域：PI3K/Akt/mTOR

作用靶點(diǎn)：PI3K

In Vitro: Risovalisib (CYH33) inhibits cell proliferation with IC₅₀s below 1?μM in 56% (18/32) of the breast cancer cell lines.
CYH33 (0.012-1 μM; for 24 hours) significantly arrests T47D and MCF7 cells in G1 phase in a concentration-dependent manner.
CYH33 (4-1000 nM; 1 hour) concurrently inhibits phosphorylation of ERK and Akt in both T47D and MCF7 cells.
CYH33 (0.11-1 μM; 24 hours) fails to induce apoptosis in MCF7 and MDA-MB-231?cells.

In Vivo: Risovalisib (CYH33) (2-20 mg/kg; oral; once a day for 21 days) potently restrains tumor growth in mice bearing human breast cancer cell xenografts.
Single administration of CYH33 (20?mg/kg; oral) significantly down-regulates the level of phosphorylated Akt in tumor tissues, demonstrating the suppression of PI3K signaling in nude mice.
CYH33 (10?mg/kg; oral; once a day for 18-d or 20-d respectively) delays the restoration of blood glucose and area under the curve (AUC) of blood glucose increased upon CYH33 treatment in T47D xenografts and R26-Pik3ca^H1047R;MMTV-Cre mice.

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