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IA4290 ARS-1620 细胞周期 索莱宝

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  • ¥780 - 4680
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  • 北京
  • IA4290
  • 2025年12月18日
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    • 详细信息
    • 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
    CASNo.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
    MDLMFCD31619312
    SMILESC=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 VitroARS-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

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    图标文献和实验
    该产品被引用文献

    【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

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