LY2606368_DataSheet_MedChemExpress
核酸聚丙烯酰胺凝胶电泳
PAGE胶的配制（DNA电泳用）50ml体系：丙烯酰胺有效分离（bp)丙烯酰胺30%（ml）10×TBE（ml)ddH2O（ml）TEMED（µl）过硫酸铵10%（µl）3.5% 100-1000 5.83 5 39.17 25.0 250 5.0% 100-500 8.33 5 36.67 25.0 250 8.0% 60-400 13.33 5 31.67 25.0 250 12.0% 40-200 20.0 5 25.00 25.0 250 15.0% 25-150 25.0 5 20.00 25.0 250 20.0% 5-100 33.33 5 11.67 25.0 250 5ml体系：丙烯酰胺丙烯酰胺30%（ml）10×TBE（ml）ddH2O（µl）TEMED（µl）过硫酸铵10%（µl）3.5% 0.583 0.5 3.917 2.5 255.0% 0.833 0.5 3.667 2.5 258.0% 1.333 0.5 3.167 2.5 25 12.0% 2.00 0.5 2.5 2.5 25 15.0% 2.50 0.5 2.0 2.5 25 20.0% 3.333 0.5 1.167 2.5 251、丙烯酰胺30%为29：1（质量比，丙烯酰胺：双甲叉丙烯酰胺）2、TEMED 可以加到1ul/ml。
不同浓度丙烯酰胺和DNA的有效分离范围表丙烯酰胺(%) 有效分离范围(bp) 溴酚兰* 二甲苯青*3.5 100～2000 100 4605.0 80～500 65 2608.0 60～400 45 16012.0 40～200 30 7015.0 25～150 15 6020.0 10～100 12 45*表中给出的数字为与指示剂迁移率相等的双链DNA分子所含碱基对数目(bp). 凝胶的制备过程：1、按要求装配好垂直电泳板，两块玻璃板的两侧及底部用1%的琼脂糖封边，防止封闭不严而使聚丙烯酰胺液漏出。
APD668_SDS_MedChemExpress
Inhibitors, Agonists, Screening LibrariesSafety Data Sheet Revision Date:Jul.-18-2017Print Date:Jul.-18-20171. PRODUCT AND COMPANY IDENTIFICATION1.1 Product identifierProduct name :APD668Catalog No. :HY-15565CAS No. :832714-46-21.2 Relevant identified uses of the substance or mixture and uses advised againstIdentified uses :Laboratory chemicals, manufacture of substances.1.3 Details of the supplier of the safety data sheetCompany:MedChemExpress USATel:609-228-6898Fax:609-228-5909E-mail:sales@1.4 Emergency telephone numberEmergency Phone #:609-228-68982. HAZARDS IDENTIFICATION2.1 Classification of the substance or mixtureNot a hazardous substance or mixture.2.2 GHS Label elements, including precautionary statementsNot a hazardous substance or mixture.2.3 Other hazardsNone.3. COMPOSITION/INFORMATION ON INGREDIENTS3.1 SubstancesSynonyms:APD 668; APD–668Formula:C21H24FN5O5SMolecular Weight:477.51CAS No. :832714-46-24. FIRST AID MEASURES4.1 Description of first aid measuresEye contactRemove any contact lenses, locate eye-wash station, and flush eyes immediately with large amounts of water. Separate eyelids with fingers to ensure adequate flushing. Promptly call a physician.Skin contactRinse skin thoroughly with large amounts of water. Remove contaminated clothing and shoes and call a physician.InhalationImmediately relocate self or casualty to fresh air. If breathing is difficult, give cardiopulmonary resuscitation (CPR). Avoid mouth-to-mouth resuscitation.IngestionWash out mouth with water; Do NOT induce vomiting; call a physician.4.2 Most important symptoms and effects, both acute and delayedThe most important known symptoms and effects are described in the labelling (see section 2.2).4.3 Indication of any immediate medical attention and special treatment neededTreat symptomatically.5. FIRE FIGHTING MEASURES5.1 Extinguishing mediaSuitable extinguishing mediaUse water spray, dry chemical, foam, and carbon dioxide fire extinguisher.5.2 Special hazards arising from the substance or mixtureDuring combustion, may emit irritant fumes.5.3 Advice for firefightersWear self-contained breathing apparatus and protective clothing.6. ACCIDENTAL RELEASE MEASURES6.1 Personal precautions, protective equipment and emergency proceduresUse full personal protective equipment. Avoid breathing vapors, mist, dust or gas. Ensure adequate ventilation. Evacuate personnel to safe areas.Refer to protective measures listed in sections 8.6.2 Environmental precautionsTry to prevent further leakage or spillage. Keep the product away from drains or water courses.6.3 Methods and materials for containment and cleaning upAbsorb solutions with finely-powdered liquid-binding material (diatomite, universal binders); Decontaminate surfaces and equipment by scrubbing with alcohol; Dispose of contaminated material according to Section 13.7. HANDLING AND STORAGE7.1 Precautions for safe handlingAvoid inhalation, contact with eyes and skin. Avoid dust and aerosol formation. Use only in areas with appropriate exhaust ventilation.7.2 Conditions for safe storage, including any incompatibilitiesKeep container tightly sealed in cool, well-ventilated area. Keep away from direct sunlight and sources of ignition.Recommended storage temperature:Powder-20°C 3 years4°C 2 yearsIn solvent-80°C 6 months-20°C 1 monthShipping at room temperature if less than 2 weeks.7.3 Specific end use(s)No data available.8. EXPOSURE CONTROLS/PERSONAL PROTECTION8.1 Control parametersComponents with workplace control parametersThis product contains no substances with occupational exposure limit values.8.2 Exposure controlsEngineering controlsEnsure adequate ventilation. Provide accessible safety shower and eye wash station.Personal protective equipmentEye protection Safety goggles with side-shields.Hand protection Protective gloves.Skin and body protection Impervious clothing.Respiratory protection Suitable respirator.Environmental exposure controls Keep the product away from drains, water courses or the soil. Cleanspillages in a safe way as soon as possible.9. PHYSICAL AND CHEMICAL PROPERTIES9.1 Information on basic physical and chemical propertiesAppearance White to off-white (Solid)Odor No data availableOdor threshold No data availablepH No data availableMelting/freezing point No data availableBoiling point/range No data availableFlash point No data availableEvaporation rate No data availableFlammability (solid, gas)No data availableUpper/lower flammability or explosive limits No data availableVapor pressure No data availableVapor density No data availableRelative density No data availableWater Solubility No data availablePartition coefficient No data availableAuto-ignition temperature No data availableDecomposition temperature No data availableViscosity No data availableExplosive properties No data availableOxidizing properties No data available9.2 Other safety informationNo data available.10. STABILITY AND REACTIVITY10.1 ReactivityNo data available.10.2 Chemical stabilityStable under recommended storage conditions.10.3 Possibility of hazardous reactionsNo data available.10.4 Conditions to avoidNo data available.10.5 Incompatible materialsStrong acids/alkalis, strong oxidising/reducing agents.10.6 Hazardous decomposition productsUnder fire conditions, may decompose and emit toxic fumes.Other decomposition products - no data available.11.TOXICOLOGICAL INFORMATION11.1 Information on toxicological effectsAcute toxicityClassified based on available data. For more details, see section 2Skin corrosion/irritationClassified based on available data. For more details, see section 2Serious eye damage/irritationClassified based on available data. For more details, see section 2Respiratory or skin sensitizationClassified based on available data. For more details, see section 2Germ cell mutagenicityClassified based on available data. For more details, see section 2CarcinogenicityIARC: No component of this product present at a level equal to or greater than 0.1% is identified as probable, possible or confirmed human carcinogen by IARC.ACGIH: No component of this product present at a level equal to or greater than 0.1% is identified as a potential or confirmed carcinogen by ACGIH.NTP: No component of this product present at a level equal to or greater than 0.1% is identified as a anticipated or confirmed carcinogen by NTP.OSHA: No component of this product present at a level equal to or greater than 0.1% is identified as a potential or confirmed carcinogen by OSHA.Reproductive toxicityClassified based on available data. For more details, see section 2Specific target organ toxicity - single exposureClassified based on available data. For more details, see section 2Specific target organ toxicity - repeated exposureClassified based on available data. For more details, see section 2Aspiration hazardClassified based on available data. For more details, see section 212. ECOLOGICAL INFORMATION12.1 ToxicityNo data available.12.2 Persistence and degradabilityNo data available.12.3 Bioaccumlative potentialNo data available.12.4 Mobility in soilNo data available.12.5 Results of PBT and vPvB assessmentPBT/vPvB assessment unavailable as chemical safety assessment not required or not conducted.12.6 Other adverse effectsNo data available.13. DISPOSAL CONSIDERATIONS13.1 Waste treatment methodsProductDispose substance in accordance with prevailing country, federal, state and local regulations.Contaminated packagingConduct recycling or disposal in accordance with prevailing country, federal, state and local regulations.14. TRANSPORT INFORMATIONDOT (US)This substance is considered to be non-hazardous for transport.IMDGThis substance is considered to be non-hazardous for transport.IATAThis substance is considered to be non-hazardous for transport.15. REGULATORY INFORMATIONSARA 302 Components:No chemicals in this material are subject to the reporting requirements of SARA Title III, Section 302.SARA 313 Components:This material does not contain any chemical components with known CAS numbers that exceed the threshold (De Minimis) reporting levels established by SARA Title III, Section 313.SARA 311/312 Hazards:No SARA Hazards.Massachusetts Right To Know Components:No components are subject to the Massachusetts Right to Know Act.Pennsylvania Right To Know Components:No components are subject to the Pennsylvania Right to Know Act.New Jersey Right To Know Components:No components are subject to the New Jersey Right to Know Act.California Prop. 65 Components:This product does not contain any chemicals known to State of California to cause cancer, birth defects, or anyother reproductive harm.16. OTHER INFORMATIONCopyright 2017 MedChemExpress. The above information is correct to the best of our present knowledge but does not purport to be all inclusive and should be used only as a guide. The product is for research use only and for experienced personnel. It must only be handled by suitably qualified experienced scientists in appropriately equipped and authorized facilities. The burden of safe use of this material rests entirely with the user. MedChemExpress disclaims all liability for any damage resulting from handling or from contact with this product.Caution: Product has not been fully validated for medical applications. For research use only.Tel: 609-228-6898 Fax: 609-228-5909 E-mail: tech@Address: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA。
ITE_448906-42-1_DataSheet_MedChemExpress
Caution: Not fully tested. For research purposes only Medchemexpress LLC
m o c . s s e r p x e m e h c d e Am S. Uw ,w 2 5w 8: 8b 0e JW Nm ,o n c o. i s t c s e nr up Jx he t m u oe h mc nd oe Mm D@ 2o 0f n 1i el : t i i a u Sm ,E e v i r D k r a P r e e D 1 1
Product Data Sheet
Product Name: CAS No.: Cat. No.: MWt: Formula: Purity :
ITE 448906-42-1 HY-19317 286.31 C14H10N2O3S &g0 mM in DMSO
Mechanisms: Pathways:Others; Target:Others g y Biological Activity: ITE is a aryl hydrocarbon receptor (AhR) agonist with Ki of 3 nM, and the estimated IC50 of ITE for OVCAR-3 cell proliferation was 0.2 nM. IC50 value: 0.2?nM (for OVCAR-3 cell), 3 nM (Ki) [1] Target: AhR in vitro: ITE is the endogenous high-affinity AhR agonist, possesses potent anticancer activity but the mechanism of action remains unclear. ITE enhances the binding of the AhR to the promoter of Oct4 and suppresses its transcription. ITE is presumably high enough in exerting its biological [1] ] functions. [ in vivo: ITE is a potential compound to induce functional FoxP3+ Treg in vivo and treat autoimmune diseases.[2]... References: [1]. Cheng J, et al. Tryptophan derivatives regulate the transcription of Oct4 in stem-like cancer cells. Nat Commun. 2015 Jun 10;6:7209. [2]. Quintana FJ, et al. An endogenous aryl hydrocarbon receptor ligand acts on dendritic cells and T cells to suppress pp experimental p autoimmune encephalomyelitis. p y Proc Natl Acad Sci U S A. 2010 Nov 30;107(48):20768-20773.
过硫酸氢钾复合物粉的制备及其相关性能研究
作者简介：周德刚（1981—），男，河南安阳，硕士，高级兽医师，从事新兽药的开发与研究，高级兽医师。
*通讯作者：李朋朋，从事新兽药的开发与研究，E-mail ：135****6019@ 。
过硫酸氢钾复合物粉的制备及其相关性能研究周德刚，李朋朋*，师梦超，杨会鲜，杨绒娟（洛阳惠中兽药有限公司，国家兽用药品工程技术研究中心河南洛阳471003）了评价过硫酸氢钾复合物粉的稳定性及其消毒效果，开展了过硫酸氢钾复合物粉的影响因素试验、加速试验及其对大肠杆菌、金黄色葡萄球菌的杀灭效果评价试验。
稳定性试验结果表明过硫酸氢钾复合物粉高温、光照试验及加速试验中，pH 、干燥失重、氯化钠、外观性状未发生变化，有效氯含量稍有降低，但含量变化在5%范围内，但在高湿条件下发生了严重结块现象，且各质量指标出现显著变化。
消毒效果评价试验表明过硫酸氢钾复合物粉800倍稀释时，对大肠杆菌、金黄色葡萄球菌的杀菌率均为100%，对大肠杆菌的最低有效浓度为1,600倍稀释，该浓度的最短作用时间为60min ；过硫酸氢钾复合物粉对金黄色葡萄球菌的最低有效浓度为1,600倍稀释，该浓度的最短作用时间为30min。
硫酸氢钾复合物粉；稳定性；细菌定量试验；细菌定性试验自2018年8月以来非洲猪瘟在我国大部分省份暴发流行，2020年2月在湖南又发生了高致病性禽流感疫情，因此畜禽养殖业中的生物安全防控工作日益严峻，人们对消毒剂的使用越来越重视，其中以过硫酸氢钾复合盐为主成分的消毒剂因其具有广谱高效、低毒环保等特点而受到广泛关注。
过硫酸氢钾复合盐消毒剂具有较强的氧化能力，在水中经过链式反应连续产生活性氧，干扰病原体的DNA 和RNA 合成，从而杀灭病原体[1]，1989年它被美国EPA 批准用于预防杀灭多种细菌和病毒的高效消毒剂，2005年被美国农业部用于机场出入境消毒，目前已在美国、英国等几十个国家上市，被广泛应用于各型农场、环境、饮水设备和空气消毒。
大麦VQ_基因家族鉴定及表达分析
54卷大麦VQ基因家族鉴定及表达分析倪守飞1，母景娇1，耿梓瀚1，王孜逸2，丛钰莹1，王月雪1，刘梦迪1，蔡倩1，赵彦宏1*，王艳芳2*（1鲁东大学农学院，山东烟台264025；2鲁东大学生命与科学学院，山东烟台264025）摘要：【目的】鉴定大麦VQ基因家族成员并进行表达分析，为大麦VQ基因的功能挖掘提供理论依据。
【方法】从大麦基因组中鉴定VQ基因家族成员，利用生物信息学方法对其结构特征及编码蛋白序列进行分析，基于转录组测序数据及实时荧光定量PCR方法进行大麦组织表达模式、盐胁迫和生物胁迫分析。
【结果】在大麦基因组中鉴定出29个HvVQ 基因（HvVQ1~HvVQ29），HvVQ蛋白序列平均长度较短（214aa），多数HvVQ蛋白为碱性或偏中性蛋白，HvVQ基因不均地分布在大麦染色体上，定位于细胞核中。
29个HvVQ蛋白均含有保守基序FxxxVQxhTG，近90%的HvVQ基因不含内含子。
进化分析将大麦、拟南芥与水稻的VQ基因家族成员分为7个亚族（Ⅰ~Ⅶ），HvVQs基因不均地分布在Ⅱ~Ⅶ亚族中。
大麦与水稻的共线性基因对数（17对）远多于与拟南芥的共线性基因对数（1对），种内共线性分析发现1对共线性基因对，非同义替换率/同义替换率（Ka/Ks）计算发现HvVQ蛋白主要处于纯化选择状态。
HvVQ基因启动区富含生长发育作用元件、非生物胁迫反应元件和激素反应元件，种类及分布均呈多样性。
对蛋白网络预测分析推断其与HvWRKY的2类亚族（Ⅱ-c和Ⅲ）存在互作关系。
大多数HvVQ基因在组织中表达，HvVQ19在受到盐胁迫时表达量明显上调，在根尖和根伸长区表达量分别上调1.40和1.10倍；对其中10个HvVQ基因进行实时荧光定量PCR检测，HvVQ2基因在蚜虫和黄矮病毒胁迫下表达量均显著下调（倍数变化<0.5为显著抑制，>2.0为显著诱导），HvVQ7和HvVQ15基因在蚜虫和黄矮病毒胁迫下表达量上调最显著，其他7个HvVQ基因也均表现出差异表达。
marker说明书
CERTIFICATE OF ANALYSISPageRuler ™Prestained Protein Ladder#SM067210 x 250 µl(for 100 mini gel applications 5 µl per well or 50 large gel applications 10 µl per well)Lot: Expiry Date:Storage: stable at 4°C for up to 3 months. For long term storage, store at -20°C.SM067_57_9.docDescriptionPageRuler ™Prestained Protein Ladder is a mixture of 10 recombinant, highly purified colored proteins with apparent molecular weights of 10 kDa to 170 kDa. Ladder proteins are covalently coupled with a blue dye except for two reference bands prestained with different colors. The 72 kDa reference band is orange and 10 kDa reference band is green.The ladder is supplied in gel loading buffer and isready-to-use: no heating, further dilution or addition of a reducing agent is required.ContentsApproximately 0.1-0.2 mg/ml of each protein in the storage buffer (62.5 mM Tris-H 3PO 4 (pH 7.5 at 25°C), 1 mM EDTA, 2% (w/v) SDS, 10 mM DTT, 1 mM NaN 3 and 33% (v/v) glycerol).Applications∙ Monitoring of protein separation during SDS-PAGE (1). ∙ Verifying Western transfer efficiency (2, 3).∙ Approximate sizing of proteins on SDS-polyacrylamidegels and Western blots.Instruction for Use❶ Thaw the ladder at room temperature for a few minutes to dissolve precipitated solids. DO NOT BOIL!❷ Mix gently, but thoroughly, to ensure the solution is homogeneous.❸ Load the following volumes of the ladder on an SDS-polyacrylamide gel:– 5 µl per well for mini gel,– 10 µl per well for large gel.Use the same volumes for Western blotting.❹ After the run is complete, stain the gel or perform Western transfer procedure as desired.Note•Each lot of the PageRuler™ Prestained Protein Ladder is calibrated against a precisely sized, PageRuler™ Unstained Protein Ladder and calculated apparent molecular weights are reported in the picture.•For precise molecular weight determinations use PageRuler™ Unstained Protein Ladder, #SM0661, see.•In 8 or 10% gels low molecular weight proteins may migrate with the dye front.•Loading volumes are intended for use in gels with a thickness of 0.75 mm. For thicker gels, the recommended loading volume should be increased.•PageRuler™ Prestained Protein Ladder could be used in Western blotting with all common membranes: PVDF, nylon and nitrocellulose.•Longer transfer times or higher transfer voltages may be required for Western blotting of large (>100 kDa) proteins.Lot specific MW, kDa4-20% Tris-glycine SDS-PAGEcontinued on back pageQUALITY CONTROL5 µl of PageRuler™ Prestained Protein Ladder resolves 10 bands of equal intensities in 4-20% SDS-PAGE (Tris-glycine buffer) and after Western blotting onto PVDF membrane.Quality authorized by: Jurgita Zilinskiene References1. Laemmli, U.K., Cleavage of structural proteins during the assembly of the head of bacteriophage T4, Nature, 227, 680-685, 1970.2. Burnette, W.N., "Western blotting": electrophoretic transfer of proteins from sodium dodecyl sulfate – polyacrylamide gels to unmodified nitrocellulose and radiographic detection with antibody and radioiodinated protein A, Anal. Biochem., 112 (2), 195-203, 1981.3. Towbin, H., et al., E lectrophoretic transfer of proteins from polyacrylamide gels to nitrocellulose sheets: procedure and some applications, Proc. Natl. Acad. Sci. USA, 76, 4350-4354, 1979.This product is manufactured under the license forStrep-tag® technology covered by US patents Nos.5,506,121, 6,103,493 and foreign counterparts. Related Products∙DualColor™ Protein Loading Buffer Pack #R1011∙Loading Buffer Pack #R0891∙Spectra™ Multicolor Broad Range Protein Ladder #SM1841∙PageRuler™ Unstained #SM0661∙PageRuler™ Plus Prestained Protein Ladder #SM1811∙PageSilver™ Silver Staining Kit #K0681∙PageBlue™ Protein Staining Solution #R0571∙10X Tris-glycine-SDS Buffer #B46∙10X Tris-tricine-SDS Buffer #B48∙DTT #R0861 ∙ProteoJET™ Mammalian Cell Lysis Reagent #K0301∙ProteoJET™ Cytoplasmic and Nuclear ProteinExtraction Kit #K0311∙Bradford Reagent, ready-to-use #R1271∙Bovine Serum Albumin Standard Set, ready-to-use #R1281∙Bovine Gamma Globulin Standard Set, ready-to-use #R1291PRODUCT USE LIMITATION.This product is developed, designed and sold exclusively for research purposes andin vitro use only. The product was not tested for use in diagnostics or for drugdevelopment, nor is it suitable for administration to humans or animals.Please refer to for Material Safety Data Sheet of the product.。
单环刺螠转录因子基因Sp8的克隆_原核表达和重组蛋白纯化_史晓丽
第４３卷 第５期 ２０１３年５月 中国海洋大学学报ＰＥＲＩＯＤＩＣＡＬ ＯＦ ＯＣＥＡＮ ＵＮＩＶＥＲＳＩＴＹ ＯＦ ＣＨＩＮＡ４３（５）：０５２～０５８Ｍａｙ，２０１３单环刺螠转录因子基因Ｓｐ８的克隆、原核表达和重组蛋白纯化＊史晓丽，刘晓龙，张立涛，张志峰＊＊（中国海洋大学海洋生物遗传育种教育部重点实验室，山东青岛２６６００３）摘 要： 转录因子Ｓｐ是一类广泛存在的锌指蛋白超家族成员，可与某些基因的上游调控序列结合，参与基因的转录调控。
本研究采用同源克隆和ＲＡＣＥ技术，获得单环刺螠的Ｓｐ８的全长ｃＤＮＡ，该序列长１ ９１３ｂｐ，开放阅读框１ ５２１ｂｐ，编码５０６个氨基酸；将其开放阅读框ｃＤＮＡ克隆到原核表达载体ｐＥＴ２８ａ中，并转化大肠杆菌ＢＬ２１（ＤＥ３）感受态细胞，在３７℃条件下，经１ｍｍｏｌ／Ｌ ＩＰＴＧ诱导表达４ｈ，获得以包涵体形式存在的重组蛋白ｐＥＴ２８ａ－ＳＰ，使用８ｍｏｌ／Ｌ尿素溶解包涵体，并通过镍离子金属螯合柱纯化获得重组蛋白，ＳＤＳ－ＰＡＧＥ分析该蛋白的分子量约为５０ｋＤ。
Ｓｐ８蛋白体外表达的成功将为研究单环刺螠相关基因的转录调控打下基础。
关键词： 单环刺螠；Ｓｐ８；转录因子；克隆；原核表达中图法分类号： Ｑ７８６ 文献标志码： Ａ 文章编号： １６７２－５１７４（２０１３）０５－０５２－０７ 转录因子Ｓｐ（Ｓｐｅｃｉｆｉｃｉｔｙ ｐｒｏｔｅｉｎ）是锌指蛋白超家族中的一个家族，参与细胞增殖、分化、凋亡以及肿瘤发生等多种生理、病理过程［１］。
该家族显著的序列特点是：羧基末端高度保守，含有３个串联的Ｃｙｓ２Ｈｉｓ２锌指结构，能结合ＤＮＡ上的ＣＡＣＣＣ元件或ＧＣ盒等序列；氨基末端在不同的家族成员间差异较大，主要是通过结合辅助因子发挥转录调控作用［２］。
迄今已发现多种Ｓｐ蛋白［３］，不同物种中Ｓｐ蛋白的种类以及参与调控的基因种类和生物学功能调控均存在差异［４］。
转录因子Ｓｐ８是Ｓｐ家族成员之一，其Ｎ端有一个丝氨酸／苏氨酸富集区，羧基端有３个串联的锌指结构和１个Ｂｔｄ ｂｏｘ。
LY2606368_CHK1抑制剂_1234015-52-1_Apexbio
参考文献: [1] Wu W, Bi C, Bence A K, et al. Antitumor activity of Chk1 inhibitor LY2606368 as a single agent in SW1990 human pancreas orthotopic tumor model. Cancer Research, 2012, 72(8 Supplement): 1776. [2] Lainchbury M, Matthews T P, McHardy T, et al. Discovery of 3-alkoxyamino-5-(pyridin-2-ylamino) pyrazine-2-carbonitriles as selective, orally bioavailable CHK1 inhibitors. Journal of medicinal chemistry, 2012, 55(22): 10229-10240. [3] McNeely S C, Burke T F, DurlandBusbice S, et al. Abstract A108: LY2606368, a second generation Chk1 inhibitor, inhibits growth of ovarian carcinoma xenografts either as monotherapy or in combination with standard-of-care agents. Molecular Cancer Therapeutics, 2011, 10(Supplement 1: Cas No.: 分子量: 分子式:
LY2606368 1234015-52-1 365.39 C18H19N7O2
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Inhibitors, Agonists, Screening Libraries
Data Sheet
BIOLOGICAL ACTIVITY:
LY2606368 is a potent and selective ATP competitive inhibitor of the Chk1 protein kinase, with a K i of 0.9 nM against purified CHK1.IC50 & Target: Ki: 0.9 nM (CHK1)[1]
In Vitro: LY2606368 results in the rapid appearance of TUNEL and pH2AX–positive double–stranded DNA breaks in the S–phase cell population. In cell assays measuring CHK1 activity through autophosphorylation of serine 296 induced by Doxorubicin or
Gemcitabine, LY2606368 has an EC 50 of <1 nM. LY2606368 potently abrogates the G2–M checkpoint activated by doxorubicin in p53–deficient HeLa cells with an EC 50 of 9 nM. In cell assays, LY2606368 does inhibit DNA damage–induced CHK2
autophosphorylation with an IC 50 of less than 31 nM. However, 100 nM LY2606368 does not inhibit PMA–stimulated RSK but instead weakly stimulates phosphorylation of S6 on serines 235/236. LY2606368 is broadly antiproliferative with IC 50 values typically <50nM in the most sensitive cell lines with a minority of cell lines showing considerable resistance with IC 50's >1,000 nM. LY2606368 (4nM) results in a large shift in cell–cycle populations from G1 and G2–M to S–phase with an accompanied induction of H2AX phosphorylation in U–2 OS cells [1].
In Vivo: LY2606368 (15 mg/kg, s.c.) shows similar activity in xenograft tumor models with less animal weight loss, which results in significant tumor growth inhibition [1].
PROTOCOL (Extracted from published papers and Only for reference)
Animal Administration: LY2606368 is formulated in vehicle consisting of 20% Captisol [1].[1]Mice [1]
Female CD–1 nu–/nu– mice (26–28 g) are used for this study. Tumor growth is initiated by subcutaneous injection of 1×106 Calu–6cells in a 1:1 mixture of serum–free growth medium and Matrigel in the rear flank of each subject animal. When tumor volumes reach approximately 150 mm 3 in size, the animals are randomized by tumor size and body weight, and placed into their respective
treatment groups. Vehicle consisting of 20% Captisol pH4 or LY2606368 is administered by subcutaneous injection in a volume of 200μL. Four, eight, 12, 24, and 48 hours after drug administration, blood for plasma drug exposure is extracted via cardiac puncture and assayed on a Sciex API 4000 LC/MS–MS system. The xenograft tissue is promptly removed and prepared. Lysates are analyzed by immunoblot analysis for protein phosphorylation levels. Group means, SEs and P values are calculated using Kronos.
References:
[1]. King C, et al. LY2606368 Causes Replication Catastrophe and Antitumor Effects through CHK1–Dependent Mechanisms. Mol Cancer Ther. 2015 Sep;14(9):2004–13
Product Name:
LY2606368Cat. No.:
HY-18174CAS No.:
1234015-52-1Molecular Formula:
C 18H 19N 7O 2Molecular Weight:
365.39Target:
Checkpoint Kinase (Chk)Pathway:
Cell Cycle/DNA Damage Solubility:
DMSO: ≥ 60 mg/mL
Caution: Product has not been fully validated for medical applications. For research use only.
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