产品
编 号：F745544
分子式：C25H33F3N8O8S2
分子量：694.7
分子式：C25H33F3N8O8S2
分子量：694.7
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
结构图
CAS No: 1494684-33-1
产品详情
生物活性：
CYH33 methanesulfonate is an orally active, highly selective PI3Kα inhibitor with IC50s of 5.9 nM/598 nM/78.7 nM/225 nM against α/β/δ/γ isoform, respectively. CYH33 methanesulfonate inhibits phosphorylation of Akt, ERK and induces significant G1 phase arrest in breast cancer cells and non-small cell lung cancer (NSCLC) cells. CYH33 methanesulfonate has potent activity against solid tumors.
体内研究：
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-Pik3caH1047R;MMTV-Cre mice. Animal Model:SCID mice aged 4-6 weeks bearing human breast cancer T47D xenografts
Dosage:2, 5, 10, 20 mg/kg
Administration:Oral; once a day for 21 days
Result:Displayed marginal inhibitory effect on the tumor growth at lower doses (2 and 5?mg/kg) and significantly attenuated tumor growth at the dose of 10 or 20?mg/kg, yielding T/C values of 58.36% and 49.42% respectively.
体外研究：
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.
CYH33 methanesulfonate is an orally active, highly selective PI3Kα inhibitor with IC50s of 5.9 nM/598 nM/78.7 nM/225 nM against α/β/δ/γ isoform, respectively. CYH33 methanesulfonate inhibits phosphorylation of Akt, ERK and induces significant G1 phase arrest in breast cancer cells and non-small cell lung cancer (NSCLC) cells. CYH33 methanesulfonate has potent activity against solid tumors.
体内研究：
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-Pik3caH1047R;MMTV-Cre mice. Animal Model:SCID mice aged 4-6 weeks bearing human breast cancer T47D xenografts
Dosage:2, 5, 10, 20 mg/kg
Administration:Oral; once a day for 21 days
Result:Displayed marginal inhibitory effect on the tumor growth at lower doses (2 and 5?mg/kg) and significantly attenuated tumor growth at the dose of 10 or 20?mg/kg, yielding T/C values of 58.36% and 49.42% respectively.
体外研究：
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.
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