| 货号 | 15279-50mg |
| 描述 | The phosphatidylinositol 3-kinase (PI3K) signaling pathway has central roles in cell growth, development, and survival.1,2 CAL-101 is a cell permeable inhibitor of the PI3K catalytic subunit p110δ (IC50 = 2.5 nM) that demonstrates 40- to 300-fold selectivity against other PI3K class I enzymes (IC50s = 820, 565, and 89 nM for p110α, β, and γ, respectively).3 At 1 μM it can block constitutive PI3K signaling in malignant B-cell lines and primary patient tumor cells, resulting in decreased phosphorylation of Akt and other downstream effectors, an increase in poly(ADP-ribose) polymerase, and apoptosis.3 It has also been shown to inhibit the chemotaxis of chronic lymphocytic leukemia cells and to downregulate the secretion of chemokines triggered by B-cell receptor signaling.4 |
| 别名 | GS-1101; Idelalisib; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Hennessy, B.T.,Smith, D.L.,Ram, P.T., et al. Exploiting the PI3K/AKT pathway for cancer drug discovery. Nature Reviews.Drug Discovery 4, 988-1004 (2005). 2.Hirsch, E.,Ciraolo, E.,Ghigo, A., et al. Taming the PI3K team to hold inflammation and cancer at bay. Pharmacology & Therapeutics 118, 192-205 (2008). 3.Lannutti, B.H.,Meadows, S.A.,Hermann, S.E.M., et al. CAL-101, a p110δ selective phosphatidylinositol-3-kinase inhibitor for the treatment of B-cell malignancies, inhibits PI3K signaling and cellular viability. Blood 117(2), 591-594 (2011). 4.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 118(13), 3603-3612 (2011). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 415.4 |
| 分子式 | C22H18FN7O |
| CAS号 | 870281-82-6 |
| 稳定性 | ≥ 2 years |
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