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CYH33 methanesulfonate

CAS No. : 1494684-33-1

MCE 站：CYH33 methanesulfonate

产品活性：CYH33 methanesulfonate 是一种具有口服活性的，高选择性 PI3Kα 抑制剂，对 α/β/δ/γ 亚型的 IC₅₀ 分别为 5.9 nM/598 nM/78.7 nM/225 nM。CYH33 methanesulfonate 抑制 Akt 和 ERK 的磷酸化，并显着诱导乳腺癌和非小细胞肺癌 (NSCLC) 细胞 G1 期阻滞。CYH33 methanesulfonate 具有有效的抗实体瘤的活性。

研究领域：PI3K/Akt/mTOR

作用靶点：PI3K

In Vitro: CYH33 methanesulfonate 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) methanesulfonate significantly arrests T47D ａnd MCF7 cells in G1 phase in a concentration-dependent manner.
CYH33 (4-1000 nM; 1 hour) methanesulfonate concurrently inhibits phosphorylation of ERK ａnd Akt in both T47D ａnd MCF7 cells.
CYH33 (0.11-1 μM; 24 hours) methanesulfonate fails to induce apoptosis in MCF7 ａnd MDA-MB-231 cells.

In Vivo: CYH33 (2-20 mg/kg; oral; once a day for 21 days) methanesulfonate potently restrains tumor growth in mice bearing human breast cancer cell xenografts.
Single administration of CYH33 (20 mg/kg; oral) methanesulfonate 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) methanesulfonate 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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