CAL-130 - CAS:1431697-74-3 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	CAL-130
英文名称:	CAL-130
别名:	2-[(1S)-1-[(2-amino-7H-purin-6-yl)amino]ethyl]-5-methyl-3-(2-methylphenyl)quinazolin-4-one
CAS No:	1431697-74-3	分子式:	C₂₃H₂₂N₈O	分子量:	426.47
CAS No:	1431697-74-3
分子式:	C₂₃H₂₂N₈O
分子量:	426.47

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C11564 CAL-130 (psaitong)

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包装规格：

5mg in glass bottle

产品描述：

基本信息

产品编号：	C11564
产品名称：	CAL-130
CAS:	1431697-74-3	储存条件	粉末	-20℃	四年
分子式：	C23H22N8O		溶于液体	-80℃	四年
分子量：	426.47
化学名：	2-[(1S)-1-[(2-amino-7H-purin-6-yl)amino]ethyl]-5-methyl-3-(2-methylphenyl)quinazolin-4-one
Solubility (25°C)：
体外:	DMSO
	Ethanol
	Water
体内(现配现用):
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。

生物活性

产品描述	一种 PI3Kδ和PI3Kγ抑制剂。
靶点	p110δ 1.3nM (IC50)	p110γ 6.1nM (IC50)	p110β 56nM (IC50)	p110α 115nM (IC50)
体外研究	CAL-130 preferentially inhibits the function of both p110γ and p110δ catalytic domains.IC50 values of CAL-130 are 1.3 and 6.1nM for p110δand p110γ,respectively,as compared to 115 and 56nM for p110αand 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.
体内研究	The clinical significance of interfering with the combined activities of PI3Kγ and PI3Kδ is determined by administering CAL130 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 45,000μL -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 (10mg/kg) of CAL-130 every 8hr for a period of 7 days and are then followed until moribund.Despite the limited duration of therapy,CAL130 is highly effective in extending the median survival for treated animals to 45 days as compared 7.5 days for the control group.

推荐实验方法(仅供参考)

激酶实验：

IC50 values for CAL-130 inhibition of PI3K isoforms are determined in ex vivo PI3 kinase assays using recombinant PI3K.A ten-point kinase inhibitory profile is determined with ATP at a concentration consistent with the KM for each enzyme.

细胞实验:

Cell proliferation of CCRF-CEM cells or shRNA-transfected CCRF-CEM cells,in presence or absence of CAL-130 (1,2.5 and 5μM),is followed by cell counting of samples in triplicate using a hemocytometer and trypan blue.For apoptosis determinations of untransfected or shRNA-transfected CCRF-CEMs,cells are stained with APC-conjugated Annexin-V in Annexin Binding Buffer and analyzed by flow cytometry.For primary T-ALL samples,cell viability is assessed using the BD Cell Viability kit coupled with the use of fluorescentcounting beads.For this,cells are plated with MS5-DL1 stroma cells,and after 72hr following CAL-130 treatment,cells are harvested and stained with an APC-conjugated antihuman CD45 followed by a staining with the aforementioned kit.

动物实验:

Mice

For subcutaneous xenograft experiments,luminescent CCRF-CEM (CEMluc) cells are generated by lentiviral infection with FUW-luc and selection with Neomycin.Luciferase expression is verified with the Dual-Luciferase Reporter Assay kit.2.5×106 CEM-luc cells embedded in Matrigel are injected in the flank of NOD.Cg-Prkdcscid Il2rgtm1Wjl/Sz mice.After 1 week,mice are treated by oral gavage with vehicle (0.5% methyl cellulose,0.1% Tween 80),or CAL-130 (10mg/kg) every 8hr daily for 4 days,and then tumors are imaged as follows:mice anesthetized by isoflurane inhalation are injected intraperitoneally with Dluciferin (50mg/kg).Photonic emission is imaged with the in vivo imaging system.Tumor bioluminescence is quantified by integrating the photonic flux (photons per second) through a region encircling each tumor using the Living Image software package.Administration of D-luciferin and detection of tumor bioluminescence in Lck/Ptenfl/fl/Gt(ROSA)26Sortm1(Luc)Kael/J mice are performed in a similar manner

保存条件：

-20℃

UN码：

HazardClass：

危害声明：

安全说明：

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