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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
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
CAL-130 是一种PI3KδPI3Kγ抑制剂,IC50分别为 1.3 和 6.1 nM。
生物活性

CAL-130 is aPI3KδandPI3Kγinhibitor withIC50s of 1.3 and 6.1 nM, respectively.

IC50& Target[1]

p110δ

1.3 nM (IC50)

p110γ

6.1 nM (IC50)

p110β

56 nM (IC50)

p110α

115 nM (IC50)

体外研究
(In Vitro)

CAL-130 preferentially inhibits the function of both p110γ and p110δ catalytic domains. IC50values 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].

体内研究
(In Vivo)

The clinical significance of interfering with the combined activities of PI3Kγ and PI3Kδ is determined by administering CAL-130 toLck/Ptenfl/flmice 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].

分子量

426.47

Formula

C23H22N8O

CAS 号

1431697-74-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.