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CYH33 methanesulfonate

产品编号 T38979 CAS 1494684-33-1

别名: CYH33 methanesulfonate

CYH33 methanesulfonate is a highly selective and orally active inhibitor of PI3Kα, with IC50 values of 5.9 nM, 598 nM, 78.7 nM, and 225 nM against the α, β, δ, and γ isoforms, respectively. This compound effectively inhibits the phosphorylation of Akt and ERK, leading to a significant G1 phase arrest in breast cancer cells and non-small cell lung cancer (NSCLC) cells. Additionally, CYH33 methanesulfonate demonstrates potent activity against solid tumors.

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CYH33 methanesulfonate Chemical Structure

CYH33 methanesulfonate, CAS 1494684-33-1

规格	价格/CNY		货期	数量
5 mg	￥ 7,890		待询
10 mg	￥ 12,300		待询

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其他形式的 CYH33 methanesulfonate:

CYH33
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参考文献

产品描述	CYH33 methanesulfonate is a highly selective and orally active inhibitor of PI3Kα, with IC50 values of 5.9 nM, 598 nM, 78.7 nM, and 225 nM against the α, β, δ, and γ isoforms, respectively. This compound effectively inhibits the phosphorylation of Akt and ERK, leading to a significant G1 phase arrest in breast cancer cells and non-small cell lung cancer (NSCLC) cells. Additionally, CYH33 methanesulfonate demonstrates potent activity against solid tumors.
靶点活性	PI3Kγ:225 nM (IC50), PI3Kα:5.9 nM (IC50), PI3Kβ:598 nM (IC50), PI3Kδ:78.7 nM (IC50)
体外活性	CYH33 methanesulfonate inhibits cell proliferation with IC 50 s below 1?μM in 56% (18/32) of the breast cancer cell lines[2]. CYH33 (0.012-1 μM; for 24 hours) methanesulfonate significantly arrests T47D and MCF7 cells in G1 phase in a concentration-dependent manner[2]. CYH33 (4-1000 nM; 1 hour) methanesulfonate concurrently inhibits phosphorylation of ERK and Akt in both T47D and MCF7 cells[2]. CYH33 (0.11-1 μM; 24 hours) methanesulfonate fails to induce apoptosis in MCF7 and MDA-MB-231?cells[2]. Cell Cycle Analysis[2]Cell Line: Sensitive T47D, MCF7 and resistant MDA-MB-231 cells Concentration: 0.012, 0.037, 0.11, 0.33, 1 μM Incubation Time: For 24 hours Result: Arrested T47D and MCF7 cells in G1 phase in a concentration-dependent manner, accompanied with concomitant reduced cell population in S phase. Had little effect on cell cycle distribution in resistant MDA-MB-231?cells. Western Blot Analysis[2]Cell Line: Sensitive T47D, MCF7 and resistant MDA-MB-231 cells Concentration: 4, 12, 37, 111, 333, 1000 nM Incubation Time: 1 hour Result: Concurrently inhibited phosphorylation of ERK and Akt in both T47D and MCF7 cells, whereas it had little effect on phosphorylated ERK (pERK) in MDA-MB-231?cells up to 1?μM.
体内活性	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[2]. 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[2]. 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[2]. Animal Model: SCID mice aged 4-6 weeks bearing human breast cancer T47D xenografts[2]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.

别名	CYH33 methanesulfonate
分子量	694.7
分子式	C25H33F3N8O8S2
CAS No.	1494684-33-1

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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参考文献

1. Haoyue Xiang, et al. Abstract LB-268: Discovery of clinical candidate methyl (5-(6-((4-(methylsulfonyl)piperazin-1-yl)methyl)-4-morpholinopyrrolo[2,1-f][1,2,4]triazin-2-yl)-4-(trifluoromethyl)pyridin-2-yl)carbamate (CYH33) : A highly potent and selective PI3K alpha inhibitor for the treatment of advanced solid tumors. AACR Annual Meeting 2018; April 14-18, 2018 2. Xue-Ling Liu, et al. Decrease in Phosphorylated ERK Indicates the Therapeutic Efficacy of a Clinical PI3Kα-selective Inhibitor CYH33 in Breast Cancer. Cancer Lett. 2018 Oct 1;433:273-282. 3. Yuxiang Wang, et al. Simultaneous inhibition of PI3Kα and CDK4/6 synergistically suppresses KRAS-mutated non-small cell lung cancer. Cancer Biol Med. 2019 Feb;16(1):66-83.

剂量换算

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体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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