化合物 Rabusertib|T6084

Rabusertib
911222-45-2

￥269 1mg 起订

￥629 5mg 起订

￥987 10mg 起订

上海更新日期：2024-09-14

TargetMol中国（陶术生物）

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联系人：邵小姐

电话：021-021-33632979拨打

手机：15002134094 拨打

邮箱：marketing@targetmol.com

产品详情:

中文名称：: 化合物 Rabusertib

英文名称：: Rabusertib

CAS号：: 911222-45-2

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：: 99.63%

产品类别：: 抑制剂

货号：: T6084

Product Introduction

Bioactivity

Name	Rabusertib
Description	Rabusertib (IC-83) is an inhibitor of the cell cycle checkpoint kinase 1 (chk1) with potential chemopotentiating activity. Rabusertib has been used in trials studying the treatment of Cancer, Solid Tumors, Advanced Cancer, Pancreatic Neoplasms, and Non-Small Cell Lung Cancer.
Cell Research	LY2603618 is prepared in DMSO (10 mM) and stock, and then diluted 1000-fold into medium[1]. Cells are plated at 2.5×103 per well, on 96-well tissue culture plates and incubated for one cell doubling (18-24 h). Gemcitabine dilutions are set up by half-log steps across a final concentration range of 1-1000 nM. LY2603618 is prepared by dilutions in DMSO to 5000× final concentration, and then diluted 1000-fold into medium to generate 5× stocks for addition to wells. Approximately 24 h after Gemcitabine addition, LY2603618 is added. Each combination is done in triplicate. After a period of two cell doublings following LY2603618 addition, MTS/PMS reagent is added to each well according to the manufacturer's instructions. Absorbance is read on a Spectra Max 250 spectrophotometer at 490 nm and the data analyzed with GraphPad Prism 4.0. Dose-response curves are fit by non-linear regression, with bottom fits constrained to 0 % inhibition[1].
Kinase Assay	Protein kinase assays are performed variously. Assays are performed on the following protein kinases: ABL, AKT1, ARG, CAMK2, CDK1, CDK2, CHK1, CHK2, DAPK1, EGFR, EPHA1, EPHB2, EPHB3, EPHB4, ERK1, ERK2, FES, FGFR1, FGFR3, FGFR4, FGR, HCK, HER2, INSR, JNK1, JNK2, LCK, MET, NTRK1, NTRK2, p38α, p38β, p38δ, p38γ, p70S6K, PDGFRα, PDGFRβ, PDK1, PKCα, ROCK2, ROS, RSK2, SGK1, SRC, SYK, TAK1, TYRO3, VEGFR2, VEGFR3, YES, ZAP70[1].
In vitro	Chk1是一个依赖ATP的丝氨酸-苏氨酸激酶，是由双链断裂(DSBs)激活的DNA复制监控检查点系统的关键成分。Chk1对所有当前定义的细胞周期检查点，包括G1/S、S期内、G2/M以及有丝分裂纺锤体检查点，都有贡献。通过抑制chk1的活性，Rabusertib阻止了DNA损伤修复过程，从而增强了各种化疗化合物的抗肿瘤效果。然而，关于Rabusertib的临床前数据直到现在还未发布。[1]预计抑制Chk1会增强抗代谢物的效果，例如gemcitabine。[2]Rabusertib治疗会损害DNA合成，增加DNA损伤（通过有丝分裂缺陷），诱导细胞凋亡，特别是在p53突变的肿瘤细胞中，与pemetrexed有协同作用。[3]
In vivo	在异种移植模型中，LY2603618与pemetrexed联合应用时可延缓肿瘤生长。[3]
Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
Solubility Information	DMSO : 4.36 mg/mL (10 mM), Sonication is recommended. H2O : < 1 mg/mL (insoluble or slightly soluble) Ethanol : < 1 mg/mL (insoluble or slightly soluble)
Keywords	inhibit \| Inhibitor \| Autophagy \| Rabusertib \| IC 83 \| Checkpoint Kinase (Chk) \| LY 2603618 \| IC83 \| LY-2603618
Inhibitors Related	Oxyresveratrol \| Guanidine hydrochloride \| Naringin \| Taurine \| Gefitinib \| Xylitol \| Hydroxychloroquine \| Curcumin \| Stavudine \| Myricetin \| Paeonol \| Sodium 4-phenylbutyrate
Related Compound Libraries	Inhibitor Library \| Anti-Cancer Active Compound Library \| Bioactive Compound Library \| Bioactive Compounds Library Max \| Kinase Inhibitor Library \| Anti-Aging Compound Library \| Highly Selective Inhibitor Library \| Drug Repurposing Compound Library \| Anti-Cancer Clinical Compound Library \| Anti-Cancer Drug Library

LY2603618|||IC-83|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

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