CAL-101 (Idelalisib, GS-1101)
| 规格 | 价格 | 货期 | 数量 |
|---|---|---|---|
| 1mL(10 mM in DMSO) | ￥545.00 | 现货 | |
| 5mg | ￥345.00 | 现货 | |
| 20mg | ￥772.00 | 现货 | |
| 50mg | ￥1181.00 | 现货 | |
| 100mg | ￥2000.00 | 现货 |
特色产品
- 适用于流式细胞仪和荧光显微镜检测
- 准确区分活细胞/凋亡细胞/坏死细胞
- 用于免疫印迹和质谱分析等后续操作
- 适用于30 KDa-130 KDa大小的蛋白
- 对细胞无毒性
- 步骤更简单，无需有机溶剂
- 可将信号灵敏度提高100倍
- 同时保持稳定的特异性和分辨率
- 提供更高的转录效率并抑制免疫激活
- 使用5-moUTP和Cy5-utp修饰
- 优异的扩增效率、可重复性和稳定性
- 卓越的灵敏度和准确性，操作简单
- 优化的缓冲液和T7 RNA聚合酶混合物
- 20 μL反应体系可获得更高的RNA产量
产品描述
CAL-101（Idelalisib，GS-1101）是一个选择性的PI3K（磷脂酰肌醇-3-激酶）p110δ的抑制剂。
PI3K p110δ可以被促进恶性B细胞增殖和存活的细胞表面受体信号所激活。CAL-101可以阻断持续性的PI3K信号，减少Akt及其它下游效应因子的磷酸化，增加聚（ADP-核糖）聚合酶（PARP)和caspase加工，诱导细胞凋亡。这些效果可以在一系列未成熟和成熟B细胞的恶性肿瘤中观察到。此外，CAL-101拮抗B细胞活化因子CD40L、TNF-α和纤连蛋白诱导的对自发凋亡的抑制。
参考文献：
Brian J. Lannutti, Sarah A. Meadows, Sarah E. M. Herman, Adam Kashishian, Bart Steiner, Amy J. Johnson, John C. Byrd, Jeffrey W. Tyner, Marc M. Loriaux, Mike Deininger, Brian J. Druker, Kamal D. Puri, Roger G. Ulrich, and Neill A. Giese. CAL-101, a p110δ selective phosphatidylinositol-3-kinase inhibitor for the treatment of B-cell malignancies, inhibits PI3K signaling and cellular viability. Blood. 2011; 117(2): 591 – 594.
Sarah E. M. Herman, Amber L. Gordon, Amy J. Wagner, Nyla A. Heerema, Weiqiang Zhao, Joseph M. Flynn, Jeffrey Jones, Leslie Andritsos, Kamal D. Puri, Brian J. Lannutti, Neill A. Giese, Xiaoli Zhang, Lai Wei, John C. Byrd, Amy J. Johnson. Phosphatidylinositol 3-kinase-δ inhibitor CAL-101 shows promising preclinical activity in chronic lymphocytic leukemia by antagonizing intrinsic and extrinsic cellular survival signals. Blood. 2010; 116(12): 2078 – 88.
产品性质
| 物理外观 | A solid |
| CAS号 | 870281-82-6 |
| 分子式 | C22H18FN7O |
| 分子量 | 415.43 |
| 小分子别名 | Idelalisib |
| 化学名称 | 5-fluoro-3-phenyl-2-[(1S)-1-(7H-purin-6-ylamino)propyl]quinazolin-4-one |
| 溶解度 | insoluble in H2O; ≥2.1 mg/mL in EtOH with gentle warming and ultrasonic; ≥80.2 mg/mL in DMSO |
| SMILES | CCC(C(N1c2ccccc2)=Nc2cccc(F)c2C1=O)Nc1ncnc2c1[nH]cn2 |
| 存储条件 | -20°C |
| 运输条件 | 蓝冰 |
产品应用 (实验数据来自文献，APExBIO并未验证，仅供参考)
IC50和靶点
| 生物活性描述 | CAL-101 (Idelalisib, GS-1101)是一个选择性的p110δ抑制剂，IC50值为2.5 nM。 |
| 靶点 | p110δ |
| 生物活性数据 | 2.5 nM |
生物相关数据
质量控制
APExBIO 顾客使用本产品发表的 8 篇科研文献
- 1. Daniel Pinto-Benito, Carmen Paradela-Leal, et al. "IGF-1 regulates astrocytic phagocytosis and inflammation through the p110α isoform of PI3K in a sex-specific manner." Glia. 2022 Jun;70(6):1153-1169. PMID: 35175663
- 2. Graeme F. Murray, Daniel Guest, et al. "Single cell biomass tracking allows identification and isolation of rare targeted therapy-resistant DLBCL cells within a mixed population." Analyst. 2021 Feb 21;146(4):1157-1162. PMID: 33426547
- 3. Julia C Gutjahr, Elisabeth Bayer, et al. "CD44 Engagement Enhances Acute Myeloid Leukemia Cell Adhesion To The Bone Marrow Microenvironment By Increasing VLA-4 Avidity." Haematologica. 2020 Jul 2;haematol.2019.231944. PMID: 32616529
- 4. Wu W, Zhou G, et al. "PI3Kδ as a Novel Therapeutic Target in Pathological Angiogenesis." Diabetes. 2020;db190713. PMID: 31915155
- 5. Xin T, Han H, et al. "Idelalisib inhibits vitreous-induced Akt activation and proliferation of retinal pigment epithelial cells from epiretinal membranes." Exp Eye Res. 2019 Nov 28:107884. PMID: 31786159
- 6. Han H, Chen N, et al. "Phosphoinositide-3-kinase δ inactivation prevents vitreous-induced activation of AKT/MDM2/p53 and migration of retinal pigment epithelial cells." J Biol Chem. 2019 Aug 29. pii: jbc.RA119.010130. PMID: 31467081
- 7. Yaya Chu, Sanghoon Lee, et al. " Ibrutinib significantly inhibited Bruton’s tyrosine kinase (BTK) phosphorylation,in-vitro proliferation and enhanced overall survival in a preclinical Burkitt lymphoma (BL) model." OncoImmunology.11 Oct 2018.
- 8. Wensveen FM, Slinger E, et al. "Antigen-affinity controls pre-germinal centser B cell selection by promoting Mcl-1 induction through BAFF receptor signaling." Sci Rep. 2016 Oct 20;6:35673. PMID: 27762293
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