CAL-101 (Idelalisib, GS-1101)_PI3K抑制剂_870281-82-6_Apexbio

sales@https://www.wendangku.net/doc/10984515.html, CAL-101 (Idelalisib, GS-1101)

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CAL-101,CAL101,Idelalisib,GS-1101,GS1101

CAL-101 is a highly selective inhibitor of p110δ.

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.