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产品总数：60957
| 中文名称 |
Risovalisib
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|---|---|
| 英文名称 |
Risovalisib
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| 英文别名 |
CYH33;RCA38L4HB5;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;CYH 33;BDBM330295;Carbamic acid, N-(5-(6-((4-(methylsulfonyl)-1-piperazinyl)methyl)-4-(4-morpholinyl)pyrrolo(2,1-F)(1,2,4)triazin-2-yl)-4-(trifluoromethyl)-2-pyridinyl)-, methyl ester;Methyl N-(5-(6-((4-(methylsulfonyl)-1-piperazinyl)methyl)-4-(4-mo;Risovalisib
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| Cas No. |
1494684-28-4
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| 分子式 |
C24H29F3N8O5S
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| 分子量 |
598.60
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| 包装储存 |
Powder -20°C 3 years；4°C 2 years
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| 产品详情 |
Risovalisib (CYH33) 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。Risovalisib 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。Risovalisib 具有有效的抗实体瘤的活性。
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|---|---|
| 生物活性 |
Risovalisib (CYH33) is an orally active, highly selective PI3Kα inhibitor with IC 50 s of 5.9 nM/598 nM/78.7 nM/225 nM against α/β/δ/γ isoform, respectively. Risovalisib inhibits phosphorylation of Akt, ERK and induces significant G1 phase arrest in breast cancer cells and non-small cell lung cancer (NSCLC) cells. Risovalisib has potent activity against solid tumors.
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| 性状 |
Solid
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| IC50 & Target[1][2] |
PI3Kα 5.9 nM (IC50) PI3Kβ 598 nM (IC5
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| 体外研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
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;MMTV-Cre mice. has not independently confirmed the accuracy of these methods. They are for reference only.
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Powder -20°C 3 years；4°C 2 years
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| ClinicalTrial |
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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.
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1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。
2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。
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