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KIN-193  ≥98%

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包装规格：5mg 10mg 25mg 50mg 100mg in glass bottle
溶解性：溶于DMSO（≥ 100 mg/mL）
产品描述：基本信息 产品编号： K10100 产品名称： AZD 6482 CAS: 1173900-33-8   储存条件 粉末 -20℃ 四年     分子式： C22H24N4O4 溶于液体 -80℃ 6个月 分子量： 408.45 -20℃ 1个月 化学名：  (R)-2-((1-(7-Methyl-2-morpholino-4-oxo-4H-pyrido[1,2-a]pyrimidin-9-yl)ethyl)amino)benzoic acid;AZD6482 Solubility (25°C)：   体外:   DMSO 82mg/mL (200.75mM) Ethanol 10mg/mL (24.48mM) Water Insoluble 体内(现配现用): 30% PEG400+0.5% Tween80+5% propylene glycol 30mg/mL ＜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。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.4483mL 12.2414mL 24.4828mL 5mM 0.4897mL 2.4483mL 4.8966mL 10mM 0.2448mL 1.2241mL 2.4483mL   生物活性 产品描述 一种有效的选择性p110β抑制剂，IC50为0.69nM。 靶点 PI3K;Autophagy 体外研究 An in vitrokinase assay demonstrates that AZD 6482 (KIN-193) is highly potent in the inhibition of p110β’s kinase activity (IC50 of 0.69nM) 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).An inhibitor-kinase interaction profiling of AZD 6482 against a panel of 433 kinases using the KinomeScan approach demonstrates that AZD 6482 is highly selective in its interaction with PI3Ks.To determine whether AZD 6482 selectively targets PTE-deficient tumors, the effect of AZD 6482 is tested on cell proliferation on a large panel of 422 cancer cell lines using high-throughput tumor cell line profiling.35% of cell lines with PTEN mutations (20 out of 57) and 16% of cell lines with wild-type PTEN (58 out of 365) are sensitive to AZD 6482 with a threshold of EC50<5µM. 体内研究 To determine the pharmacodynamics of AZD 6482 (KIN-193) in tumors in vivo,rat fibroblast (Rat1) cells are engineered to express both p53DD,a dominant negative mutant of p53,and a constitutively activated myr-p110β (Rat1-CA-p110β) to enable these cells to form xenograft tumors in mice.For comparison,an isogenic Rat1 cell line expressing p53DD and myrp110α(Rat1-CA-p110α) is also generated.Rat1-CA-p110αand Rat1-CA-p110βcells are introduced subcutaneously into the contralateral flanks of athymic mice such that tumors driven by activated p110αor p110βwould be exposed to identical conditions and that concern about animal-to-animal variability could be eliminated.When tumors reach a volume of ~500 mm3,the tumor-bearing mice receives a single IP injection of AZD 6482 (10mg/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-p110αand 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-p110βtumors,but remain unchanged in Rat1-CAp110αtumors.   推荐实验方法(仅供参考) 激酶实验： AZD 6482 (KIN-193) is profiled at a concentration of 10µM against a diverse panel of 433 kinases.Scores for primary screen hits are reported as percent of the DMSO control (% control).For kinases where no score is shown,no measurable binding is detected.The lower the score,the lower the Kd is likely to be,such that scores of zero represent strong hits.Scores are related to the probability of a hit,but are not strictly an affinity measurement.At a screening concentration of 10µM,a score of less than 10% implies that the false positive probability is less than 20% and the Kd is most likely less than 1µM.A score between 1-10% implies that the false positive probability is less than 10%,although it is difficult to assign a quantitative affinity from a single-point primary screen.A score of less than 1% implies that the false positive probability is less than 5% and the Kd is most likely less than 1µM.   细胞实验:   Cell viability is determined.Briefly,cells are seeded in medium containing 5% FBS at a density insuring cell growth throughout drug treatment (~15% for most cell lines).Drug treatment is started 24h post seeding and continued for 72h.Cell are fixed and stained using Syto60,a red fluorescent DNA stain.The relative cell number is calculated by taking the ratio of the relative fluorescence intensity from drug treated wells over untreated wells after background subtraction (cells-free wells).Nine doses of AZD 6482 (KIN-193) are used in 2-fold dilution steps ranging from 5.12µM to 0.02µM.IC50,corresponding to 50% cell number compared to control (untreated) wells,is determined using a fixed top and bottom sigmoidal fitting algorithm implemented in PipelinePilot.   动物实验:   Mice Approximately 6-8 week-old female nude mice are injected s.c.with Rat1-Myr-HA-p110α(Rat1-CAp110α) cells (1×106 cells in 40% matrigel) in one flank (site 1) and Rat1-Myr-HA-p110β (Rat1-CAp110β) cells (0.5×106 cells in 10% matrigel) in the contralateral flank (site 2).When tumors grow to ~500 mm3,mice are dosed once by ip injection with AZD 6482 formulated in 7.5% NMP,40% PEG400,52.5% dH2O at 0.1mL/10g body weight and 10mg/kg.Tumors are collected at 0,1,4,8,and 24h following compound administration and blood samples are obtained by direct heart puncture.Serum is separated and stored at -80℃.The drug concentrations in serum and tumor samples are assessed by LC-MS/MS analysis by the DMPK group.
保存条件：-20℃

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