|(R)-2-((1-(7-甲基-2-吗啉基-4-氧代-4H-吡啶并[1,2-a]嘧啶-9-基)乙基)氨基)苯甲酸|CsnPharm

CAS No.: 1173900-33-8

AZD 6482 Catalog No. CSN12381

Synonyms: KIN-193

AZD6482 is a PI3Kβ inhibitor with IC50 of 10 nM, 8-, 87- and 109-fold selective to PI3Kβ than PI3Kδ, PI3Kα and PI3Kγ.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述An in vitro kinase assay demonstrates that AZD 6482 (KIN-193) is highly potent in the inhibition of p110β's kinase activity (IC50 of 0.69 nM) and has 200, 20, and 70-fold selectivity over p110α, p110δ, and p110γ isoforms, respectively. AZD 6482 also exhibits selectivity of ~80 fold over PI3K-C2β and DNA-PK and more than 1,000-fold over other phosphatidylinositol-3 kinase–related kinases (PIKKs). When tumors reach a volume of ~500 mm3, the tumor-bearing mice receives a single IP injection of AZD 6482 (10 mg/kg). The plasma concentration of AZD 6482 is highest at 1 hour post-injection and declined to undetectable levels by 4h. Concentrations of AZD 6482 in both the CA-p110α- and CA-p110β-driven tumors parallel the plasma concentrations. Analyses of tumor lysates harvested at various time points after AZD 6482 injection reveal that the phosphorylation of AKT is significantly reduced at 1hour after AZD 6482 injection in Rat1-CA-p110β tumors, but remain unchanged in Rat1-CAp110α tumors^[3]. KIN-193 is efficacious specifically in blocking AKT signaling and tumor growth that are dependent on p110β activation or PTEN loss. Broad profiling across a panel of 422 human tumor cell lines shows that the PTEN mutation status of cancer cells strongly correlates with their response to KIN-193^[3]. Further investigation on AZD6482 profile revealed that mutations in RB1, KRAS, NRAS and APC contributed in drug resistance. Changes in both AZD6482-sensitive and -resistant gene sets showed limited impact on prognosis. Western blotting showed AZD6482 did not induce changes in a panel of major downstream effectors of AKT, but substantially increased PMS2 level. AZD6482 also selectively inhibited migration, invasiveness, and colony formation of ccRCC cells with SETD2 mutations^[4].
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
human 639-V cell	-	Growth inhibition assay	-	Inhibition of human 639-V cell growth in a cell viability assay, IC50=1.63144 μM	SANGER
human 786-0 cell	-	Growth inhibition assay	-	Inhibition of human 786-0 cell growth in a cell viability assay, IC50=1.31283 μM	SANGER
human A427 cell	-	Growth inhibition assay	-	Inhibition of human A427 cell growth in a cell viability assay, IC50=0.99505 μM	SANGER

更多
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00853450	Antiplatelet Effect	Phase 1	Completed	-	Sweden ... more >> Research Site Lund, Sweden Collapse <<
NCT00688714	Antiplatelet Effect	Phase 1	Completed	-	-

参考文献

[1] Weigelt B, Warne PH, et al. PI3K pathway dependencies in endometrioid endometrial cancer cell lines. Clin Cancer Res. 2013 Jul 1;19(13):3533-44.
[2] Nylander S, Kull B, et al. Human target validation of phosphoinositide 3-kinase (PI3K)β: effects on platelets and insulin sensitivity, using AZD6482 a novel PI3Kβ inhibitor. J Thromb Haemost. 2012 Oct;10(10):2127-36.
[3] Jing Ni,et al. Functional characterization of an isoform-selective inhibitor of PI3K-p110β as a potential anticancer agent. Cancer Discov. 2012 May;2(5):425-33.
[4] Jun Wang,et al. High selectivity of PI3Kβ inhibitors in SETD2-mutated renal clear cell carcinoma. J BUON. Sep-Oct 2015;20(5):1267-75.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.4483 mL
- 12.2414 mL
- 24.4828 mL
- 5 mM
- 0.4897 mL
- 2.4483 mL
- 4.8966 mL
- 10 mM
- 0.2448 mL
- 1.2241 mL
- 2.4483 mL

技术信息

CAS号

1173900-33-8

储存条件

粉末: Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C22H24N4O4

运输

蓝冰

分子量

408.45

别名

KIN-193

溶解度

DMSO	82.0 mg/mL (200.8 mM)
Water	Insoluble
Ethanol	10.0 mg/mL (24.5 mM)

动物实验配方

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Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources

human 639-V cell	-	Growth inhibition assay	-	Inhibition of human 639-V cell growth in a cell viability assay, IC50=1.63144 μM	SANGER
human 786-0 cell	-	Growth inhibition assay	-	Inhibition of human 786-0 cell growth in a cell viability assay, IC50=1.31283 μM	SANGER
human A427 cell	-	Growth inhibition assay	-	Inhibition of human A427 cell growth in a cell viability assay, IC50=0.99505 μM	SANGER
human A498 cell	-	Growth inhibition assay	-	Inhibition of human A498 cell growth in a cell viability assay, IC50=0.11795 μM	SANGER
human Becker cell	-	Growth inhibition assay	-	Inhibition of human Becker cell growth in a cell viability assay, IC50=1.36315 μM	SANGER
human BT-20 cell	-	Growth inhibition assay	-	Inhibition of human BT-20 cell growth in a cell viability assay, IC50=0.59222 μM	SANGER
human CAMA-1 cell	-	Growth inhibition assay	-	Inhibition of human CAMA-1 cell growth in a cell viability assay, IC50=1.2001 μM	SANGER
human CCF-STTG1 cell	-	Growth inhibition assay	-	Inhibition of human CCF-STTG1 cell growth in a cell viability assay, IC50=1.42525 μM	SANGER
human COLO-684 cell	-	Growth inhibition assay	-	Inhibition of human COLO-684 cell growth in a cell viability assay, IC50=2.20032 μM	SANGER
human D-336MG cell	-	Growth inhibition assay	-	Inhibition of human D-336MG cell growth in a cell viability assay, IC50=1.6688 μM	SANGER
human D-542MG cell	-	Growth inhibition assay	-	Inhibition of human D-542MG cell growth in a cell viability assay, IC50=1.85077 μM	SANGER
human Daudi cell	-	Growth inhibition assay	-	Inhibition of human Daudi cell growth in a cell viability assay, IC50=1.06888 μM	SANGER
human EB2 cell	-	Growth inhibition assay	-	Inhibition of human EB2 cell growth in a cell viability assay, IC50=1.75019 μM	SANGER
human ES7 cell	-	Growth inhibition assay	-	Inhibition of human ES7 cell growth in a cell viability assay, IC50=0.81286 μM	SANGER
human EW-7 cell	-	Growth inhibition assay	-	Inhibition of human EW-7 cell growth in a cell viability assay, IC50=0.86356 μM	SANGER
human GDM-1 cell	-	Growth inhibition assay	-	Inhibition of human GDM-1 cell growth in a cell viability assay, IC50=2.24206 μM	SANGER
human GI-1 cell	-	Growth inhibition assay	-	Inhibition of human GI-1 cell growth in a cell viability assay, IC50=1.31808 μM	SANGER
human HAL-01 cell	-	Growth inhibition assay	-	Inhibition of human HAL-01 cell growth in a cell viability assay, IC50=1.30175 μM	SANGER
human HCC70 cell	-	Growth inhibition assay	-	Inhibition of human HCC70 cell growth in a cell viability assay, IC50=1.66146 μM	SANGER
human HGC-27 cell	-	Growth inhibition assay	-	Inhibition of human HGC-27 cell growth in a cell viability assay， IC50=1.1816 μM	SANGER
human HH cell	-	Growth inhibition assay	-	Inhibition of human HH cell growth in a cell viability assay, IC50=0.96222 μM	SANGER
human HSC-2 cell	-	Growth inhibition assay	-	Inhibition of human HSC-2 cell growth in a cell viability assay, IC50=1.75727 μM	SANGER
human HuO9 cell	-	Growth inhibition assay	-	Inhibition of human HuO9 cell growth in a cell viability assay, IC50=1.6128 μM	SANGER
human J82 cell	-	Growth inhibition assay	-	Inhibition of human J82 cell growth in a cell viability assay, IC50=0.47779 μM	SANGER
human KU812 cell	-	Growth inhibition assay	-	Inhibition of human KU812 cell growth in a cell viability assay, IC50=1.59628 μM	SANGER
human KURAMOCHI cell	-	Growth inhibition assay	-	Inhibition of human KURAMOCHI cell growth in a cell viability assay, IC50=0.1051 μM	SANGER
human LoVo cell	-	Growth inhibition assay	-	Inhibition of human LoVo cell growth in a cell viability assay, IC50=1.73825 μM	SANGER
human LXF-289 cell	-	Growth inhibition assay	-	Inhibition of human LXF-289 cell growth in a cell viability assay, IC50=1.55104 μM	SANGER
human MAD-MB-468 cells	-	Function assay	-	Inhibition of PI3Kbeta in human MAD-MB-468 cells assessed as inhibition of Ser473 Akt phosphorylation by cellular potency assay, IC50=0.04 μM	24992874
human MC116 cell	-	Growth inhibition assay	-	Inhibition of human MC116 cell growth in a cell viability assay, IC50=1.46122 μM	SANGER
human MDA-MB-361 cell	-	Growth inhibition assay	-	Inhibition of human MDA-MB-361 cell growth in a cell viability assay, IC50=3.52709 μM	SANGER
human MDA-MB-415 cell	-	Growth inhibition assay	-	Inhibition of human MDA-MB-415 cell growth in a cell viability assay, IC50=0.16732 μM	SANGER
human MDA-MB-468 cell	-	Growth inhibition assay	-	Inhibition of human MDA-MB-468 cell growth in a cell viability assay, IC50=1.53736 μM	SANGER
human MEL-HO cell	-	Growth inhibition assay	-	Inhibition of human MEL-HO cell growth in a cell viability assay, IC50=1.24238 μM	SANGER
human MFE-296 cell	-	Growth inhibition assay	-	Inhibition of human MFE-296 cell growth in a cell viability assay, IC50=1.56836 μM	SANGER
human NALM-6 cell	-	Growth inhibition assay	-	Inhibition of human NALM-6 cell growth in a cell viability assay, IC50=0.70465 μM	SANGER
human NB12 cell	-	Growth inhibition assay	-	Inhibition of human NB12 cell growth in a cell viability assay, IC50=1.54842 μM	SANGER
human NCI-H1048 cell	-	Growth inhibition assay	-	Inhibition of human NCI-H1048 cell growth in a cell viability assay, IC50=1.22579 μM	SANGER
human NCI-H1755 cell	-	Growth inhibition assay	-	Inhibition of human NCI-H1755 cell growth in a cell viability assay, IC50=3.27063 μM	SANGER
human NCI-H2030 cell	-	Growth inhibition assay	-	Inhibition of human NCI-H2030 cell growth in a cell viability assay, IC50=2.90288 μM	SANGER
human NCI-H2291 cell	-	Growth inhibition assay	-	Inhibition of human NCI-H2291 cell growth in a cell viability assay, IC50=1.5761 μM	SANGER
human NCI-H2342 cell	-	Growth inhibition assay	-	Inhibition of human NCI-H2342 cell growth in a cell viability assay, IC50=0.84294 μM	SANGER
human NCI-H650 cel	-	Growth inhibition assay	-	Inhibition of human NCI-H650 cell growth in a cell viability assay, IC50=1.30076 μM	SANGER
human NKM-1 cell	-	Growth inhibition assay	-	Inhibition of human NKM-1 cell growth in a cell viability assay, IC50=1.28636 μM	SANGER
human OCUB-M cell	-	Growth inhibition assay	-	Inhibition of human OCUB-M cell growth in a cell viability assay, IC50=1.58314 μM	SANGER
human OS-RC-2 cell	-	Growth inhibition assay	-	Inhibition of human OS-RC-2 cell growth in a cell viability assay, IC50=0.62388 μM	SANGER
human OVCAR-3 cell	-	Growth inhibition assay	-	Inhibition of human OVCAR-3 cell growth in a cell viability assay, IC50=0.67946 μM	SANGER
human P30-OHK cell	-	Growth inhibition assay	-	Inhibition of human P30-OHK cell growth in a cell viability assay, IC50=1.07138 μM	SANGER
human RPMI-6666 cell	-	Growth inhibition assay	-	Inhibition of human RPMI-6666 cell growth in a cell viability assay, IC50=0.64379 μM	SANGER
human RS4-11 cell	-	Growth inhibition assay	-	Inhibition of human RS4-11 cell growth in a cell viability assay, IC50=0.73806 μM	SANGER
human RXF393 cell	-	Growth inhibition assay	-	Inhibition of human RXF393 cell growth in a cell viability assay, IC50=0.01154 μM	SANGER
human SCC-9 cell	-	Growth inhibition assay	-	Inhibition of human SCC-9 cell growth in a cell viability assay, IC50=0.8577 μM	SANGER
human SF295 cell	-	Growth inhibition assay	-	Inhibition of human SF295 cell growth in a cell viability assay, IC50=2.76955 μM	SANGER
human SK-MES-1 cell	-	Growth inhibition assay	-	Inhibition of human SK-MES-1 cell growth in a cell viability assay, IC50=0.78967 μM	SANGER
human SK-OV-3 cell	-	Growth inhibition assay	-	Inhibition of human SK-OV-3 cell growth in a cell viability assay, IC50=1.20444 μM	SANGER
human SNB75 cell	-	Growth inhibition assay	-	Inhibition of human SNB75 cell growth in a cell viability assay, IC50=1.66508 μM	SANGER
human SNU-423 cell	-	Growth inhibition assay	-	Inhibition of human SNU-423 cell growth in a cell viability assay, IC50=1.57192 μM	SANGER
human SU-DHL-1 cell	-	Growth inhibition assay	-	Inhibition of human SU-DHL-1 cell growth in a cell viability assay, IC50=0.56813 μM	SANGER
human SW1088 cell	-	Growth inhibition assay	-	Inhibition of human SW1088 cell growth in a cell viability assay, IC50=2.48143 μM	SANGER
human SW1710 cell	-	Growth inhibition assay	-	Inhibition of human SW1710 cell growth in a cell viability assay, IC50=0.5292 μM	SANGER
human SW982 cell	-	Growth inhibition assay	-	Inhibition of human SW982 cell growth in a cell viability assay, IC50=0.03584 μM	SANGER
human T47D cell	-	Growth inhibition assay	-	Inhibition of human T47D cell growth in a cell viability assay, IC50=0.5327 μM	SANGER
human VMRC-RCZ cell	-	Growth inhibition assay	-	Inhibition of human VMRC-RCZ cell growth in a cell viability assay, IC50=0.14898 μM	SANGER
human YT cell	-	Growth inhibition assay	-	Inhibition of human YT cell growth in a cell viability assay, IC50=0.12066 μM	SANGER

AZD 6482 Catalog No. CSN12381

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