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Submit ReviewIdelalisib is a potent PI 3-Kinase δ inhibitor (IC50 = 2.5 nM for p110δ); it exhibits >40-fold selectivity for the δ isoform over other PI 3-K class I enzymes (IC50s = 89, 565, and 820 nM for p110γ, p110β, and p110α respectively). Idelalisib blocks constitutive PI 3-K signaling in malignant B-cell lines and primary patient tumor cells. Idelalisib inhibits chronic lymphocytic leukemia cell chemotaxis and downregulates chemokine secretion triggered by B-cell receptor signaling in stromal cocultures. Idelalisib lacks significant cytotoxicity toward natural killer (NK) cells. Idelalisib also decreases production of inflammatory cytokines, including TNF-γ, CD40L, and IL-6 by T cells and IFN-γ by NK cells. Idelalisib is cell-permeable and orally bioavailable.
Idelalisib is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. 了解 Tocris 化合物库的更多信息。
分子量 | 415.42 |
公式 | C22H18FN7O |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 870281-82-6 |
PubChem ID | 11625818 |
InChI Key | IFSDAJWBUCMOAH-HNNXBMFYSA-N |
Smiles | [C@H](NC1=C2C(N=CN2)=NC=N1)(CC)C=3N(C(=O)C=4C(N3)=CC=CC4F)C5=CC=CC=C5 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 41.54 | 100 | |
ethanol | 4.15 | 10 |
以下数据基于产品分子量 415.42。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.41 mL | 12.04 mL | 24.07 mL |
5 mM | 0.48 mL | 2.41 mL | 4.81 mL |
10 mM | 0.24 mL | 1.2 mL | 2.41 mL |
50 mM | 0.05 mL | 0.24 mL | 0.48 mL |
参考文献是支持产品生物活性的出版物。
Herman et al (2010) Phosphatidylinositol 3-kinase-δ inhibitor CAL-101 shows promising preclinical activity in chronic lymphocytic leukemia by antagonizing intrinsic and extrinsic cellular survival signals. Blood 116 2078 PMID: 20522708
Lannutti et al (2011) CAL-101, a p110delta selective phosphatidylinositol-3-kinase inhibitor for the treatment of B-cell malignancies, inhibits PI3K signaling and cellular viability. Blood 117 591 PMID: 20959606
Poli et al (2021) PIP4Ks impact on PI3K, FOXP3, and UHRF1 signaling and modulate human regulatory T cell proliferation and immunosuppressive activity. Proc.Natl.Acad.Sci.U.S.A. 118 e2010053118 PMID: 34312224
Hoellenriegel et al (2011) The phosphoinositide 3'-kinase delta inhibitor, CAL-101, inhibits B-cell receptor signaling and chemokine networks in chronic lymphocytic leukemia. Blood 118 3603 PMID: 21803855
If you know of a relevant reference for Idelalisib, please let us know.
关键词: Idelalisib, Idelalisib supplier, potent, selective, PI, 3-Kinase, delta, isoform, inhibitor, chronic, lymphocytic, leukemia, cell, permeable, orally, biovavailable, PI3K, 7631, Tocris Bioscience
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