艾代拉里斯|T1894|TargetMol

Idelalisib
870281-82-6

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上海更新日期：2024-09-23

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产品详情:

中文名称：: 艾代拉里斯

英文名称：: Idelalisib

CAS号：: 870281-82-6

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.94%

产品类别：: 抑制剂

货号：: T1894

Product Introduction

Bioactivity

名称	Idelalisib
描述	Idelalisib (GS-1101) is a small molecule inhibitor of the PI3K catalytic subunit p110δ (IC50: 2.5 nM). The selectivity for p110δ is 40- to 300-fold than p110α/β/γ.
细胞实验	MTT assays were performed to determine cytotoxicity. Briefly, 1 × 10^5 cells (CLL B cells or healthy volunteer T cells or NK cells) were incubated for 48 hours with different concentrations of CAL-101, 25μM LY294002, or vehicle control. MTT reagent was then added, and plates were incubated for an additional 20 hours before washing with protamine sulfate in phosphate-buffered saline. Dimethyl sulfoxide was added, and absorbance was measured by spectrophotometry at 540 nm in a Labsystems plate reader. Cell viability was also measured at various time points with the use of annexin/PI flow cytometry. Data were analyzed with Expo-ADC32 software package. At least 10 000 cells were counted for each sample. Results were expressed as the percentage of total positive cells over untreated control. Experiments examining caspase-dependent apoptosis included the addition of 100μM Z-VAD. Experiments examining survival signals included the addition of 1 μg/mL CD40L, 800 U/mL IL-4, 50 ng/mL BAFF, 20 ng/mL TNF-α, or coculturing on fibronectin or stromal (HS-5 cell line) coated plates. Stromal coculture was done by plating a 75-cm2 flask (80%-100% confluent) per 6-well plate 24 hours before the addition of CLL cells [2].
激酶实验	PI3K assay was performed on whole-cell lysates from CLL or normal B cells. A PI3K ELISA assay was performed according to the manufacturer's instructions. Briefly, whole-cell extracts were added to a mixture of PI(4,5)P2 substrate and reaction buffer containing adenosine triphosphate (ATP) and allowed to incubate at room temperature. The reaction was stopped by adding PI(3,4,5)P3 detector mixed with EDTA (ethylenediaminetetraacetic acid) and allowed to incubate at room temperature for 1 hour. After this time, the mixture was transferred from each well to a PI3K ELISA plate and allowed to incubate 1 hour. Plates were washed and then incubated with a secondary detector for 30 minutes. Plates were washed again, and 3,3′,5,5′-tetramethylbenzidine solution was added for 5 minutes at which time H2SO4 was added to stop all reactions. Plates were read at 450 nm on a Labsystems 96-well plate reader [2].
动物实验	For Idelalisib (CAL-101) treatment, wild-type C57BL/6 mice were administered either 40 mg kg 1 CAL-101 or vehicle DMSO, by 25 ml infusion into the femoral vein, 15 min before I/R (pre-treatment), or 3 and 6 h after initiation of reperfusion (post-treatment). Controls and animals treated with CAL-101 underwent cerebral blood flow (CBF) measurements using a laser Doppler perfusion monitor. The CBF measurements obtained immediately before and after MCAO and again at 3 h after reperfusion showed a B90–95% reduction in the blood flow to the MCAO infarct region, which did not differ between groups [4].
体外活性	Idelalisib 是一种口服的 p110δ 抑制剂，目前正在对 B 细胞恶性肿瘤患者进行临床评估。Idelalisib 对 p110δ 的选择性比对其他 PI3K 类 I 酶（IC50 p110δ = 2.5nM; p110α、p110β 和 p110γ 的 IC50 分别为 820、565 和 89nM）高出 40 至 300 倍。相对于 C2β、hVPS34、DNA-PK 和 mTOR 等相关激酶，其选择性更高（400 至 4000 倍），而在 10μM 浓度下对一个包含 402 种多样激酶的测试组未显示任何活性[1]。Idelalisib 能够在剂量和时间依赖的方式下促进原发性 CLL 细胞的凋亡，这一过程与常见的预后标记物无关。Idelalisib 引发的细胞毒性依赖于半胱天冬酶，并且通过在基质细胞上共培养并未减弱[2]。CAL-101 抑制 CLL 细胞向 CXCL12 和 CXCL13 的趋化以及在基质细胞下的迁移（伪包裹现象）。Idelalisib 还能下调在基质共培养和 BCR 触发后的趋化因子的分泌。Idelalisib 减少了来自 BCR 或像护士一样的细胞的生存信号，并抑制 BCR- 和趋化因子受体诱导的 AKT 和 MAP 激酶（ERK）活化[3]。
体内活性	单次静脉注射40 mg/kg的Idelalisib，于缺血前15分钟给药（预处理），在野生型小鼠中显著降低了72小时后的梗塞面积。然而，较低剂量elalisib（20、10和1 mg/kg）未能实现显著的保护效果。重要的是，即便在再灌注开始后3小时给药（治疗后），每千克体重40 mg的Idelalisib剂量仍能有效减少梗塞体积，与对照组相比平均降低了44%[4]。
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	H2O : Insoluble Ethanol : 22 mg/mL (53 mM) DMSO : 50 mg/mL (120.36 mM)
关键字	GS 1101 \| PI3K \| GS1101 \| CAL101 \| Idelalisib \| Phosphoinositide 3-kinase \| Autophagy \| Inhibitor \| inhibit \| CAL 101
相关产品	Oxyresveratrol \| Guanidine hydrochloride \| Naringin \| Taurine \| Gefitinib \| Hydroxychloroquine \| Curcumin \| Stavudine \| Paeonol \| Sodium 4-phenylbutyrate
相关库	抗癌活性化合物库 \| 已知活性化合物库 \| EMA 上市药物库 \| 激酶抑制剂库 \| 抗衰老化合物库 \| FDA 上市药物库 \| FDA 上市激酶抑制剂库 \| 药物功能重定位化合物库 \| 抗癌临床化合物库 \| 抗癌药物库

艾代拉里斯|||GS-1101|||CAL-101|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(12年)
注册资本	566.2651万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,试剂,定制,服务
主营行业	化学试剂,生物活性小分子