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CAL-130
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CAL-130图片
CAS NO:1431697-74-3
规格:98%
分子量:426.47
包装与价格:
包装价格(元)
2mg电议
5mg电议
10mg电议
50mg电议

产品介绍
CAL-130 是一种 PI3Kδ 和 PI3Kγ 抑制剂,IC50 分别为 1.3 和 6.1 nM。
CAS:1431697-74-3
分子式:C23H22N8O
分子量:426.47
纯度:98%
存储:Store at -20°C

Background:

CAL-130 is a PI3Kδ and PI3Kγ inhibitor with IC50s of 1.3 and 6.1 nM, respectively. p110δ|1.3 nM (IC50)|p110γ|6.1 nM (IC50)|p110β|56 nM (IC50)|p110α|115 nM (IC50)


CAL-130 preferentially inhibits the function of both p110γ and p110δ catalytic domains. IC50 values of CAL-130 are 1.3 and 6.1 nM for p110δ and p110γ, respectively, as compared to 115 and 56 nM for p110α and p110β. CAL-130 does not inhibit additional intracellular signaling pathways (i.e., p38 MAPK or insulin receptor tyrosine kinase) that are critical for general cell function and survival[1].


The clinical significance of interfering with the combined activities of PI3Kγ and PI3Kδ is determined by administering CAL-130 to Lck/Ptenfl/fl mice with established T cell acute lymphoblastic leukemia (T-ALL). Candidate animals for survival studies are ill appearing, have a white blood cell (WBC) count above 45,000 μL-1, evidence of blasts on peripheral smear, and a majority of circulation cells (>75%) staining double positive for Thy1.2 and Ki-67. Mice receive an oral dose (10 mg/kg) of CAL-130 every 8 hr for a period of 7 days and are then followed until moribund. Despite the limited duration of therapy, CAL-130 is highly effective in extending the median survival for treated animals to 45 days as compared 7.5 days for the control group[1].


[1]. Subramaniam Prem S, et al. Targeting nonclassical oncogenes for therapy in T-ALL. Cancer cell (2012), 21(4), 459-72.