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CAL-101 (Idelalisib, GS-1101)PI3K抑制剂

CAL-101 (Idelalisib, GS-1101)

产品编号:A3005
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规格 单价 库存 订购数量
10mM (in 1mL DMSO) ¥600.00 现货
5mg ¥500.00 现货
20mg ¥1,100.00 现货
50mg ¥1,600.00 现货
100mg ¥2,650.00 现货

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Sample solution is provided at 25 µL, 10mM.

引用文献

1. 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.
2. 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

质量控制

化学结构

CAL-101 (Idelalisib, GS-1101)

相关生物数据

CAL-101 (Idelalisib, GS-1101)

相关生物数据

CAL-101 (Idelalisib, GS-1101)

相关生物数据

CAL-101 (Idelalisib, GS-1101)

CAL-101 (Idelalisib, GS-1101) Dilution Calculator

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CAL-101 (Idelalisib, GS-1101) Molarity Calculator

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化学性质

CAS号 870281-82-6 SDF Download SDF
别名 CAL-101,CAL101,Idelalisib,GS-1101,GS1101
化学名 5-fluoro-3-phenyl-2-[(1S)-1-(7H-purin-6-ylamino)propyl]quinazolin-4-one
SMILES CCC(C1=NC2=C(C(=CC=C2)F)C(=O)N1C3=CC=CC=C3)NC4=NC=NC5=C4NC=N5
分子式 C22H18FN7O 分子量 415.43
溶解度 ≥80.2 mg/mL in DMSO, <2.09 mg/mL in H2O, ≥2.1 mg/mL in EtOH with ultrasonic and warming 储存条件 Store at -20°C
物理性状 A solid 运输条件 试用装:蓝冰运输。
其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议 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。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

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          
IC50 2.5 nM          

实验操作

细胞实验[1]:

细胞系

CD19/CD5阳性CLL细胞(> 90%)

溶解方法

在DMSO中的溶解度>10 mM。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

< 5 μM:剂量依赖地抑制anti-IgM的促存活效应;= 5 μM,24h:抑制2.6%的anti-IgM活性;> 5 μM,72h:最大限度地减少CLL细胞的活力。

应用

CAL-101在较低剂量水平(< 5 μM)以剂量依赖的方式抑制anti-IgM的促存活效应。CAL-101在大于 5 μM浓度下处理72小时后最大限度地减少CLL细胞的活力。在5 μM浓度下处理24小时后,CAL-101显著减少了2.6%的anti-IgM的平均(SEM)促存活效应(92.7%)。

动物实验[2]:

动物模型

异种移植含有JAK2突变和/或CRLF2改变的从头(n=3)或复发(n=1)儿童Ph-样ALL样本的NOD-SCID-γ-null (NSG) 小鼠。

剂量

30 mg/kg/天,3天,口服给药。

应用

CAL101治疗可以有效抑制体内相关蛋白的磷酸化,包括磷酸化的(p)PI3K、mTOR、S6和AktS473,没有观察到其它已测蛋白磷酸化的增加,表明近端抑制有效抑制异常PI3K途径的信号转导,并诱导最小的补偿性信号上调。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。

References:

[1] Hoellenriegel J, Meadows S A, Sivina M, et al. The phosphoinositide 3′-kinase delta inhibitor, CAL-101, inhibits B-cell receptor signaling and chemokine networks in chronic lymphocytic leukemia. Blood, 2011, 118(13): 3603-3612.

[2] Li Y, Ryan T, Vincent T, et al. In vivo efficacy of PI3K pathway signaling inhibition for Philadelphia chromosome-like acute lymphoblastic leukemia. Blood, 2013, 122(21): 2672-2672.

View Related Products By Research Topics

研究更新

2. The phosphoinositide 3'-kinase delta inhibitor, CAL-101, inhibits B-cell receptor signaling and chemokine networks in chronic lymphocytic leukemia. Blood. 2011 Sep 29;118(13):3603-12. doi: 10.1182/blood-2011-05-352492. Epub 2011 Jul 29.
Abstract
CAL-101 is a selective inhibitor of PI3Kδ that induces rapid lymph node shrinkage and a transient lymphocytosis in CLL cells. CAL-101 not only directly inhibits the pro-survival PI3K pathway but also disrupts CLL-microenvironment interactions, where it inhibits chemotaxis and migration of CLL cell, down-regulates BCR-induced chemokines secretion, reduces survival signals and suppresses ERK activation.
3. PI3Kδ inhibitor, GS-1101 (CAL-101), attenuates pathway signaling, induces apoptosis, and overcomes signals from the microenvironment in cellular models of Hodgkin lymphoma. Blood. 2012 Feb 23;119(8):1897-900. doi: 10.1182/blood-2011-10-386763. Epub 2011 Dec 30.
Abstract
CAL-101, an oral inhibitor of PI3Kδ, inhibited AKT phosphorylation and stroma-induced Akt activation, reduced CCL5 production and dose-dependently induced apoptosis in HL cells. Moreover, addition of everolimu could enhance the anti-HL activity of CAL-101.
4. CAL-101, a p110delta selective phosphatidylinositol-3-kinase inhibitor for the treatment of B-cell malignancies, inhibits PI3K signaling and cellular viability. Blood. 2011 Jan 13;117(2):591-4. doi: 10.1182/blood-2010-03-275305. Epub 2010 Oct 19.
Abstract
CAL-101 is an inhibitor of p110δ that blocks phosphatidylinositol-3-kinase signaling in a wide range of B-cell malignancies leading to decreased phosphorylation of Akt and other downstream effectors, increased polu(ADP-ribose) polymerase and caspase cleavage and induced apoptosis.
5. Translating PI3K-Delta Inhibitors to the Clinic in Chronic Lymphocytic Leukemia: The Story of CAL-101 (GS1101). Am Soc Clin Oncol Educ Book. 2012;32:691-694. doi: 10.14694/EdBook_AM.2012.32.691.
Abstract
CAL-101, a p110 delta inhibitor, has been developed fr the treatment of chronic lymphoid malignancies including CLL.

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.