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- 文献和实验
- 技术资料
- 保存条件:
Powder:2-8℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year
- 保质期:
Powder:2-8℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year
- 英文名:
ARS-1620
- 库存:
现询
- 供应商:
北京索莱宝科技有限公司
- CAS号:
1698055-85-4
- 规格:
25mg/10mg/1mg/5mg
| 规格: | 25mg | 产品价格: | ¥4680.0 |
|---|---|---|---|
| 规格: | 10mg | 产品价格: | ¥2880.0 |
| 规格: | 1mg | 产品价格: | ¥780.0 |
| 规格: | 5mg | 产品价格: | ¥1880.0 |
ARS-1620是一种有效的KRASG12C共价抑制剂。
【本资料源自公开渠道,如需(此处)屏蔽,请联系删除】
标题:Astaxanthin Prevents Glucocorticoid-Induced Femoral Head Osteonecrosis by Targeting Ferroptosis through the JAK2/STAT3 Signaling Pathway
成员:Yu-zhe Lin, Zi-hao Chen, Jian-feng Yang, Li-jiang Han, Yi-tian Yu, Juan-nan Zhan, Guang-chan Tan, Le-yang Liu, Cheng-long Xie, Ping Shan, Chen Jin, Hai-xiao Liu
论文因子:5.7 发表期刊:JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY pmid:39903514
【本资料源自公开渠道,如需(此处)屏蔽,请联系删除】
标题:Novel lncRNA LncMSTRG.11341.25 Promotes Osteogenic Differentiation of Human Bone Marrow Stem Cells via the miR-939-5p/PAX8 Axis
成员:Feifei Ni, Jianjun Li, Qin Yin, Yangyang Chen, Zengwu Shao, Hong Wang
论文因子:8.5 发表期刊:Research pmid:39916798
【本资料源自公开渠道,如需(此处)屏蔽,请联系删除】
标题:Multifunctional hydrogel loaded with 4-octyl itaconate and exosomes to induce bone regeneration for diabetic infected bone defect via Keap1-Nrf2 pathway
成员:Yizhou Wan, Qing Gao, Bing Ye, Wenzhe Sun, Kaifang Chen, Xiaodong Guo
论文因子:8.7 发表期刊:Materials Today Bio pmid:40070866
【本资料源自公开渠道,如需(此处)屏蔽,请联系删除】
标题:The Phase-Transited Lysozyme Coating Modified Small Intestinal Submucosa Membrane Loaded with Calcium and Zinc Ions for Enhanced Bone Regeneration
成员:Yilin Yang, Tianyi Tong, Xin Li, Hong Zheng, Shiyu Yao, Jiayin Deng, Qi Zhang, Zihao Liu, Xin Huang, Hongjie Li, Yuzhu Mu, Shiqing Ma
论文因子:10 发表期刊:Advanced Healthcare Materials pmid:39995373
【本资料源自公开渠道,如需(此处)屏蔽,请联系删除】
标题:Mussel-inspired antimicrobial hydrogel with cellulose nanocrystals/tannic acid modified silver nanoparticles for enhanced calvarial bone regeneration
成员:Xingchen Li, Yuxuan Pang, Lin Guan, Lei Li, Yanlin Zhu, Andrew K. Whittaker, Bai Yang, Song Zhu, Quan Lin
论文因子:7.7 发表期刊:INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES pmid:38759859
| 基本信息 | |
| CAS | No.1698055-85-4 |
| 英文名称 | ARS-1620 |
| 别名 | CPD-1588 |
| 分子式 | C21H17ClF2N4O2 |
| 分子量 | 430.84 |
| 溶解性 | Soluble in DMSO ≥5mg/mL(Need ultrasonic) |
| 纯度 | ≥98% |
| 外观(性状) | Off-white to yellow Solid |
| 储存条件 | Powder:2-8℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year |
| MDL | MFCD31619312 |
| SMILES | C=CC(N1CCN(C2=C3C=C(Cl)[C@@]([C@@]4=C(O)C=CC=C4F)=C(F)C3=NC=N2)CC1)=O.[S] |
| 靶点 | K-Ras |
| 通路 | Cell Cycle; GPCR & G Protein |
| 背景说明 | ARS-1620是一种有效的KRASG12C共价抑制剂。 |
| 生物活性 | ARS-1620 is an atropisomeric selective KRASG12C inhibitor with desirable pharmacokinetics.[1] |
| In Vitro | ARS-1620 is an atropisomeric selective KRASG12C inhibitor with desirable pharmacokinetics. ARS-1620 exhibits complete growth suppression of p.G12C cell lines (IC50=150 nM) with relatively benign effects on control cell lines. It is found that ARS-1620 significantly reduces expression of the gene set in p.G12C mutant cells in a time-dependent manner but not in the p.G12S mutant cells. Following a 5-day treatment period, only a minority of G12C mutant cell lines are sensitive to ARS-1620 under monolayer culture conditions, whereas in 3D-spheroid conditions, ARS-1620 elicits a robust response (p=0.0140)[1]. |
| 细胞实验 | Following a single oral dose or 5 consecutive daily doses, ARS-1620 yields average peak tumor concentrations of 1.5 μM (50 mg/kg) and 5.5 μM (200 mg/kg), respectively, that enables significant KRASG12C target occupancy (>=70% G12C-TE at 200 mg/kg) for >24 hr. In MIAPaCa2 xenografts (p.G12C), ARS-1620 significantly inhibits tumor growth[1] |
| 细胞实验 | 5×104 cells are seeded into 24 well ULA-plates and allowed to rest overnight. Cells are then treated with DMSO or ARS-1620. After 2 days of treatment, apoptosis and cell death is measured by staining with annexinV-APC and prodidium iodide or by 70% ethanol fixation followed by FxCycle Violet staining to measure DNA content (cell cycle) and percentage of sub-diploid events by flow cytometry[1]. |
| 动物实验 | For pharmacokinetic (PK) studies 6- to 8-week-old male BALB/c mice are used. To determine oral bioavailability, mice are treated with ARS-1620 by a single intravenous (IV) bolus or oral gavage administration at the doses of 2 and 10 mg/kg, respectively. ARS-1620 concentration in plasma is quantified by LC-MS/MS-based methods. Pharmacokinetic parameters are estimated from mean plasma concentration-time profiles. The area under the curve (AUC) is calculated from time versus concentration data using the linear trapezoidal rule. The oral bioavailability is calculated as the ratio of AUC for ARS-1620 from oral and IV dosage. The calculation is normalized by relative doses[1]. |
| 数据来源文献 | [1]. Janes MR, et al. Targeting KRAS Mutant Cancers with a Covalent G12C-Specific Inhibitor. Cell. 2018 Jan 25;172(3):578-589.e17. |
| 单位 | 瓶 |
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文献和实验【本资料源自公开渠道,如需(此处)屏蔽,请联系删除】
标题:Astaxanthin Prevents Glucocorticoid-Induced Femoral Head Osteonecrosis by Targeting Ferroptosis through the JAK2/STAT3 Signaling Pathway
成员:Yu-zhe Lin, Zi-hao Chen, Jian-feng Yang, Li-jiang Han, Yi-tian Yu, Juan-nan Zhan, Guang-chan Tan, Le-yang Liu, Cheng-long Xie, Ping Shan, Chen Jin, Hai-xiao Liu
论文因子:5.7 发表期刊:JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY pmid:39903514
【本资料源自公开渠道,如需(此处)屏蔽,请联系删除】
标题:Novel lncRNA LncMSTRG.11341.25 Promotes Osteogenic Differentiation of Human Bone Marrow Stem Cells via the miR-939-5p/PAX8 Axis
成员:Feifei Ni, Jianjun Li, Qin Yin, Yangyang Chen, Zengwu Shao, Hong Wang
论文因子:8.5 发表期刊:Research pmid:39916798
【本资料源自公开渠道,如需(此处)屏蔽,请联系删除】
标题:Multifunctional hydrogel loaded with 4-octyl itaconate and exosomes to induce bone regeneration for diabetic infected bone defect via Keap1-Nrf2 pathway
成员:Yizhou Wan, Qing Gao, Bing Ye, Wenzhe Sun, Kaifang Chen, Xiaodong Guo
论文因子:8.7 发表期刊:Materials Today Bio pmid:40070866
【本资料源自公开渠道,如需(此处)屏蔽,请联系删除】
标题:The Phase-Transited Lysozyme Coating Modified Small Intestinal Submucosa Membrane Loaded with Calcium and Zinc Ions for Enhanced Bone Regeneration
成员:Yilin Yang, Tianyi Tong, Xin Li, Hong Zheng, Shiyu Yao, Jiayin Deng, Qi Zhang, Zihao Liu, Xin Huang, Hongjie Li, Yuzhu Mu, Shiqing Ma
论文因子:10 发表期刊:Advanced Healthcare Materials pmid:39995373
【本资料源自公开渠道,如需(此处)屏蔽,请联系删除】
标题:Mussel-inspired antimicrobial hydrogel with cellulose nanocrystals/tannic acid modified silver nanoparticles for enhanced calvarial bone regeneration
成员:Xingchen Li, Yuxuan Pang, Lin Guan, Lei Li, Yanlin Zhu, Andrew K. Whittaker, Bai Yang, Song Zhu, Quan Lin
论文因子:7.7 发表期刊:INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES pmid:38759859
周三啦!又见面啦!一周终于过去了一半!!!读篇科研报庆祝一下吧~①什么味的西红柿好吃?科学家给你分析一下吧!现在,来自农业研究局(ARS)和Boyce Thompson研究所(BTI)的科学家们在刚刚发表的《Nature Genetics》一文中,重点讨论了这个问题。位于纽约伊萨卡的ARS植物、土壤和营养研究实验室的分子生物学家James Giovannoni和BTI生物信息学科学家Zhangjun Fei完成了栽培番茄及其野生亲缘植物的泛基因组(pan-genome)构建,绘制了近5000
科研民工救星:JAMA子刊发现它既能祛痘,还能治脱发,今日已被FDA批准上市
针对激素的外用药物。虽然口服避孕药和螺内酯联合使用是解决痤疮激素发病机制的有效选择,但这些药物有可能造成全身不良反应,且不能用于男性患者。 Clascoterone 破局 ——图片来源:JAMA Dermatology在皮脂腺内,皮脂细胞将前体分子转化为雄激素,其中包括双氢睾酮(DHT)。雄激素受体(ARs)在皮肤各处表达,并在皮脂腺、皮脂细胞和真皮乳头细胞中被发现。循环和局部(皮肤)合成的雄激素,如睾丸素和双氢睾酮(DHT)结合在皮肤上,刺激男性和女性皮脂和炎症的产生。在皮脂腺细胞中,DHT
了样品的液流技术、细胞的分选和计数技术,以及数据的采集和分析技术等。 2.细胞的参量和荧光探针 FCM 是通过测量细胞的多种参量来获取信息的,细胞参数分为结构参量和功能参量两大类。结 构参量主要用于描述细胞的化学组分和形态特征,例如DNA、RNA的含量,总蛋白含量、胞内PH值 和细胞大小等;功能参量主要是描述细胞整体的理化和生物特性,如:细胞周期动力学、特殊配体的鉴 定、特殊细胞的生物活性等,这些参量有的需要经荧光标记才能被测定,有的并不需要荧光标记[4]。 2.1参数
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