BMS-599626_AC480_Protein Tyrosine Kinase_EGFR-HER2_CAS号8173837-23-1说明书_AbMole中国
EpCAM_EpCAM蛋白_EpCAM Protein使用说明书
GMP级重组人EpCAM蛋白（冻干粉）Recombinant Human EpCAM Protein作用机理：EpCAM 是一种泛上皮分化抗原，在几乎所有的癌细胞上作为 17-1A（mAb）抗原表达。
它的组成功能正在被阐明，它与钙黏蛋白-连环蛋白途径错综复杂地连接，因此是负责细胞内信号传导和极性的基本 Wnt 途径。
上皮细胞粘附分子（EpCAM）已知在大多数上皮性恶性肿瘤中表达，并被报道为肿瘤标志物或分子靶向治疗的候选抗原。
EpCAM 与 N-钙粘蛋白的交叉信号涉及 PI3K，导致上皮细胞中钙粘蛋白粘附复合物的废除。
上皮细胞粘附分子（EpCAM ）作为乳腺癌的一种预后因子，近年来受到越来越多的关注。
规格参数：货号：TL-668 规格：50ug产品信息：表达宿主：人 HEK293 细胞同源名称：EPCAM,TACSTD1,TROP1,CD326,DIAR5,EGP2,EGP314,EGP40,ESA,GA733-2,HNPCC8,HNPCC-8,KS1/4,KSA,M4S1,MIC18,MK1蛋白序列：DNA 序列编码人 EpCAM（ NCBI Reference Sequence: NP_002345.2）表达带有 His 标签在 C 末端分子量：重组人 EpCAM 蛋白包含 241 个氨基酸，预测理论分子量为 29.1 kd纯度：≥95%采用 SDS-PAGE 凝胶和高效液相色谱分析内毒素：＜0.1EU/ug生物活性：通过固定化蛋白支持 L 细胞-小鼠成纤维细胞系黏附的能力进行测定。
当将 5×104细胞/孔添加到重组人 EpCAM 和人纤维连接蛋白涂层板（0.5μg/ml）中时，细胞粘附以剂量依赖性方式增强。
这种作用的 ED50为 1-2.4μg/ml。
纯化方式：层析纯化性状：白色疏松体保存温度：2-8℃有效期：24 个月生产厂家：同立海源生物使用说明：稳定性和储存：冻干的样本的可以在4℃保存 24 个月，溶解后的液体可以于-20℃保存 6-12 个月，并且避免反复冻融。
(完整word版)赫赛汀中文说明书
【药物名】Trastuzumab（曲妥珠单抗）【商品名】 Herceptin（赫赛汀）【批准文号】国药准字 J20110020【剂型】注射剂【形状】每瓶含浓缩曲妥珠单抗粉末440mg，为白色至淡黄色冻干粉剂。
配制成溶液后为无色或淡黄色澄清或微乳光色【类别】免疫检验点抑制剂【靶点】 Her2【分子量】约185kDa【生产公司】Genentech 罗氏子公司基因泰克【作用机理】特异结合于HER2受体胞外段从而阻断HER2同源二聚体的组成性激活并干扰HER2与其它ErbB家族成员形成异源二聚体。
介导HER2受体的内吞和在溶酶体中的降解；活化PTEN阻断PI3K信号通路；上调并活化p27kip1从而诱导G1期停滞，抑制肿瘤细胞增殖；促进肿瘤细胞凋亡；抗肿瘤血管生成；ADCC作用；抑制全长HER2受体胞外段的裂解和裂解产物p95的活化；抑制DNA修复；增加化疗药物的细胞毒性；逆转肿瘤细胞对宿主细胞因子杀伤作用的抵抗等。
【适应症和用途】赫赛汀是一种HER2/neu受体拮抗剂，主要用于治疗：•HER2过量表达的乳腺癌；•HER2过量表达的转移性胃癌或胃食管交界处腺癌。
【副反应】1. 心肌毒性2. 输注反应3. 化疗引起的中性粒细胞减少症加重4. 肺毒性赫赛汀最常见的不良反应是：发热、恶心、呕吐、输注反应、腹泻、感染、咳嗽加重、头痛、乏力、呼吸困难、皮疹、中性粒细胞减少症、贫血和肌痛。
需要中断或停止赫赛汀治疗的不良反应包括：充血性心衰、左心室功能明显下降、严重的输注反应和肺毒性。
【禁忌症】禁用于已知对赫赛汀过敏或者对任何本品其它组分过敏的患者。
【警告和注意事项】孕妇及哺乳期妇女用药：生殖研究在Cynomolgus猴子中进行，当剂量给至人每周维持剂量（2 mg/kg）的25倍时，未见明显生育力缺陷或对胎儿有害。
在发育早期（孕20-50天）和晚期（孕120-150天）均观察到赫赛汀经胎盘传送入胎儿。
赫赛汀用于妊娠妇女是否会引起胎儿损害及是否会影响生殖能力目前尚不清楚。
Bikinin_CAS号188011-69-0_M8228说明书_AbMole中国
分子量273.08溶解性（25°C）DMSO分子式C H BrN O WaterCAS号188011-69-0Ethanol储存条件3年 -20°C 粉末状生物活性Bikinin is a strong activator of brassinosteroid (BR) signaling. It is an Arabidopsis GSK-3 Inhibitor, an Arabidopsis SHAGGY-related Kinase Inhibitor, and a GSK-3-like Kinase BIN2 Inhibitor. Bikinin directly inhibits BIN2 (group II GSK3s) by interfering with ATP binding. Bikinin is specific toward a subset of Arabidopsis GSK3 kinases including BIN2 and ASK α, γ, ε, ι, and θ.不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）小鼠大鼠兔豚鼠仓鼠狗重量 (kg)0.020.15 1.80.40.0810体表面积 (m)0.0070.0250.150.050.020.5K系数36128520动物 A (mg/kg) = 动物 B (mg/kg) ×动物 B的K系数动物 A的K系数例如，依据体表面积折算法，将白藜芦醇用于小鼠的剂量22.4 mg/kg 换算成大鼠的剂量，需要将22.4 mg/kg 乘以小鼠的K系数（3），再除以大鼠的K系数（6），得到白藜芦醇用于大鼠的等效剂量为11.2 mg/kg。
Bikinin 目录号M8228化学数据99232mmmm m。
依洛尤单抗注射液Evolocumab-详细说明书与重点
依洛尤单抗注射液Evolocumab 英文名称: Evolocumab Injection【成分】依洛尤单抗是一种人单克隆免疫球蛋白G2（IgG2），针对人前蛋白转化酶枯草溶菌素kexin 9 型（PCSK9）。
依洛尤单抗的分子量（MW）大约为144 kDa，由转基因哺乳动物（中国仓鼠卵巢）细胞产生。
依洛尤单抗是一种无菌、无防腐剂、澄清至乳白、无色至淡黄色的溶液，通过皮下注射给药。
每支1 mL 一次性使用的预充式SureClick®自动注射器含140 mg 依洛尤单抗、醋酸（1.2 mg）、聚山梨醇酯80（0.1 mg）、脯氨酸（25 mg），溶于注射用水，USP 中。
可使用氢氧化钠调节pH 至5.0。
【性状】依洛尤单抗是一种无菌、无色至淡黄色澄明液体，可带轻微乳光。
【适应症】纯合子型家族性高胆固醇血症：用于成人或12岁以上青少年的纯合子型家族性高胆固醇血症；可与饮食疗法和其他降低密度脂蛋白（LDL）的治疗（例如他汀类药物、依折麦布、LDL分离术）合用，用于患有纯合子型家族性高胆固醇血症（HoFH）且需要进一步降低低密度脂蛋白胆固醇（LDL-C）的患者。
用于成人动脉粥样硬化性心血管疾病（ASCVD）的治疗，以降低心肌梗死、卒中和冠状动脉血运重建的风险。
【规格】1mL:140mg (预充式自动注射笔)【用法用量】皮下给药。
使用一次性预充式自动注射器，在腹部、大腿或上臂非柔嫩、淤青、红肿或变硬的部位通过皮下注射给予依洛尤单抗。
对于HoFH 患者，依洛尤单抗的推荐皮下给药剂量为420 mg 每月1 次。
鉴于对治疗的应答取决于LDL-受体功能的水平，应在依洛尤单抗给药4-8 周后检测HoFH 患者的LDL-C 水平。
如果错过每月1 次的给药，应指导患者：•错过给药时间在7 天以内，给予依洛尤单抗，并继续使用以前的给药时间表。
•错过给药时间超过7 天，给予依洛尤单抗，并基于这次给药时间重新计划给药时间表。
碧云天生物技术聚甲基丙烯酸2-羟乙酯产品说明书
碧云天生物技术/Beyotime Biotechnology 订货热线：400-168-3301或800-8283301 订货e-mail ：******************技术咨询：*****************网址：碧云天网站 微信公众号聚甲基丙烯酸2-羟乙酯(BioPlus)产品编号 产品名称包装 ST1582-1g 聚甲基丙烯酸2-羟乙酯(BioPlus) 1g ST1582-5g 聚甲基丙烯酸2-羟乙酯(BioPlus) 5g ST1582-25g聚甲基丙烯酸2-羟乙酯(BioPlus)25g产品简介：CAS Number Chemical FormulaMolecular WeightPurity Grade 25249-16-5(C 6H 10O 3)n--BioPlus基本信息(General Information)：Name (Chinese) 聚甲基丙烯酸2-羟乙酯 Name (English) Poly(2-hydroxyethyl methacrylate) Specifications BioPlus, suitable for cell culture Chemical Formula (C 6H 10O 3)n Synonym (Chinese) 聚(2-HEMA), 聚-HEMA Synonym (English) Poly(2-HEMA); Poly-HEMA Beilstein Registry No. - EINECS Number - MDL Number MFCD00084374 UNSPSC Code 12352200 产品描述(Description)： Application 用于抑制细胞对培养容器中生长表面的粘附。
Physical form 遇水膨胀聚合物。
水凝胶。
性质(Properties)：density 1.15g/mL at 25°C(lit.) solubility ethanol: soluble120mg/mL form powdersuitabilitysuitable for cell culture安全信息(Safety Information)：Hazard Pictogram Codes- Signal Word - Hazard Statements - Precautionary Statements-Personal Protective Equipment Eyeshields, Gloves, type N95 (US), type P1 (EN143) respirator filter Hazard Codes (Europe) - Risk Codes (Europe) - Safety Codes (Europe)-RIDADR NONH for all modes of transport WGK Germany3 RTECS - Flash Point (F) - Flash Point (C)-包装清单:产品编号 产品名称包装 ST1582-1g聚甲基丙烯酸2-羟乙酯(BioPlus)1gST1582-5g 聚甲基丙烯酸2-羟乙酯(BioPlus) 5gST1582-25g 聚甲基丙烯酸2-羟乙酯(BioPlus) 25g－说明书1份保存条件：室温保存。
重组人Syk蛋白产品说明书
Product datasheetRecombinant Human Syk protein ab1527191 图像描述产品名称重组人Syk蛋白表达系统Wheat germAccession P43405蛋白长度Protein fragment无动物成分No性质Recombinant种属Human序列HYSYKADGLLRVLTVPCQKIGTQGNVNFGGRPQLPGSHPATWSAGGIISRIKSYSFPKPGHRKSSPAQGNRQESTVSFNPYEPELAPWAADKGPQREA预测分子量37 kDa including tags氨基酸243 to 340技术指标Our Abpromise guarantee covers the use of ab152719 in the following tested applications.The application notes include recommended starting dilutions; optimal dilutions/concentrations should be determined by the end user.应用SDS-PAGEWestern blotELISA形式Liquid补充说明Protein concentration is above or equal to 0.05 µg/µl.Best use within three months from the date of receipt of this protein.制备和贮存稳定性和存储Shipped on dry ice. Upon delivery aliquot and store at -80ºC. Avoid freeze / thaw cycles.pH: 8.00Constituents: 0.31% Glutathione, 0.79% Tris HCl常规信息功能Non-receptor tyrosine kinase which mediates signal transduction downstream of a variety oftransmembrane receptors including classical immunoreceptors like the B-cell receptor (BCR).Regulates several biological processes including innate and adaptive immunity, cell adhesion,osteoclast maturation, platelet activation and vascular development. Assembles into signalingcomplexes with activated receptors at the plasma membrane via interaction between its SH2domains and the receptor tyrosine-phosphorylated ITAM domains. The association with thereceptor can also be indirect and mediated by adapter proteins containing ITAM or partialhemITAM domains. The phosphorylation of the ITAM domains is generally mediated by SRCsubfamily kinases upon engagement of the receptor. More rarely signal transduction via SYKcould be ITAM-independent. Direct downstream effectors phosphorylated by SYK include VAV1,PLCG1, PI-3-kinase, LCP2 and BLNK. Initially identified as essential in B-cell receptor (BCR)signaling, it is necessary for the maturation of B-cells most probably at the pro-B to pre-Btransition. Activated upon BCR engagement, it phosphorylates and activates BLNK an adapterlinking the activated BCR to downstream signaling adapters and effectors. It also phosphorylatesand activates PLCG1 and the PKC signaling pathway. It also phosphorylates BTK and regulatesits activity in B-cell antigen receptor (BCR)-coupled signaling. In addition to its functiondownstream of BCR plays also a role in T-cell receptor signaling. Plays also a crucial role in theinnate immune response to fungal, bacterial and viral pathogens. It is for instance activated by themembrane lectin CLEC7A. Upon stimulation by fungal proteins, CLEC7A together with SYKactivates immune cells inducing the production of ROS. Also activates the inflammasome and NF-kappa-B-mediated transcription of chemokines and cytokines in presence of pathogens.Regulates neutrophil degranulation and phagocytosis through activation of the MAPK signalingcascade. Also mediates the activation of dendritic cells by cell necrosis stimuli. Also involved inmast cells activation. Also functions downstream of receptors mediating cell adhesion. Relays forinstance, integrin-mediated neutrophils and macrophages activation and P-selectinreceptor/SELPG-mediated recruitment of leukocytes to inflammatory loci. Plays also a role in non-immune processes. It is for instance involved in vascular development where it may regulate bloodand lymphatic vascular separation. It is also required for osteoclast development and function.Functions in the activation of platelets by collagen, mediating PLCG2 phosphorylation andactivation. May be coupled to the collagen receptor by the ITAM domain-containing FCER1G.Also activated by the membrane lectin CLEC1B that is required for activation of platelets byPDPN/podoplanin. Involved in platelet adhesion being activated by ITGB3 engaged by fibrinogen.组织特异性Widely expressed in hematopoietic cells (at protein level). Within the B-cells compartment it is forinstance expressed for pro-B-cells to plasma cells.序列相似性Belongs to the protein kinase superfamily. Tyr protein kinase family. SYK/ZAP-70 subfamily.Contains 1 protein kinase domain.Contains 2 SH2 domains.结构域The SH2 domains mediate the interaction of SYK with the phosphorylated ITAM domains oftransmembrane proteins. Some proteins like CLEC1B have a partial ITAM domain (also calledhemITAM) containing a single YxxL motif. The interaction with SYK requires CLEC1Bhomodimerization.翻译后修饰Ubiquitinated by CBLB after BCR activation; which promotes proteasomal degradation.Autophosphorylated. Phosphorylated on tyrosine residues by LYN following receptorsengagement. Phosphorylation on Tyr-323 creates a binding site for CBL, an adapter protein thatserves as a negative regulator of BCR-stimulated calcium ion signaling. Phosphorylation at Tyr-348 creates a binding site for VAV1. Phosphorylation on Tyr-348 and Tyr-352 enhances thephosphorylation and activation of phospholipase C-gamma and the early phase of calcium ionmobilization via a phosphoinositide 3-kinase-independent pathway (By similarity).Phosphorylation on Ser-297 is very common, it peaks 5 minutes after BCR stimulation, andcreates a binding site for YWHAG. Phosphorylation at Tyr-630 creates a binding site for BLNK.Dephosphorylated by PTPN6.细胞定位Cell membrane. Cytoplasm, cytosol.SDS-PAGE - Recombinant Human Syk protein (ab152719)12.5% SDS-PAGE stained with Coomassie Blue.图片Please note: A ll products are "FOR RESEA RCH USE ONLY. NOT FOR USE IN DIA GNOSTIC PROCEDURES"Our Abpromise to you: Quality guaranteed and expert technical supportReplacement or refund for products not performing as stated on the datasheetValid for 12 months from date of deliveryResponse to your inquiry within 24 hoursWe provide support in Chinese, English, French, German, Japanese and SpanishExtensive multi-media technical resources to help youWe investigate all quality concerns to ensure our products perform to the highest standardsIf the product does not perform as described on this datasheet, we will offer a refund or replacement. For full details of the Abpromise, please visit https:///abpromise or contact our technical team.Terms and conditionsGuarantee only valid for products bought direct from Abcam or one of our authorized distributors。
YK-4-279_Cell Cycle_DNA-RNA Synthesis_CAS号1037184-44-3说明书_AbMole中国
分子量366.2溶解性（25°C ）DMSO分子式C H Cl NO Water <1 mg/mL CAS 号1037184-44-3Ethanol <1 mg/mL储存条件3年 -20°C 粉末状生物活性YK 4-279是RNA 解旋酶A （RHA ）与致癌转录因子EWS-FLI1结合抑制剂，能抑制ESFT 细胞增长，诱导凋亡。
YK-4-279 validates the splicing mechanism of EWS-FLI1, showing alternatively spliced gene patterns that significantly overlap with EWS-FLI1 reduction and WT human mesenchymal stem cells (hMSC). YK-4-279inhibits ERG and ETV1 biological activity in fusion-positive prostate cancer cells leading to decreased motility and invasion. Therefore, YK-4-279 may have an impact on metastasis in prostate cancer and it may be further evaluated for its clinical applications in prostate cancer in addition to Ewing's sarcoma.实验操作 来自于公开的文献，仅供参考细胞实验细胞系方法浓度处理时间动物实验动物模型Nude mice bearing prostate cancer PC3, TC71 or CHP-100 xenografts 配制DMSO 剂量 1.5 mg/dose 给药处理i.p.不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA 指南）小鼠大鼠兔豚鼠仓鼠狗重量 (kg)0.020.15 1.80.40.0810体表面积 (m )0.0070.0250.150.050.020.5K 系数36128520动物 A (mg/kg) = 动物 B (mg/kg) ×动物 B 的K 系数动物 A 的K 系数例如，依据体表面积折算法，将白藜芦醇用于小鼠的剂量22.4 mg/kg 换算成大鼠的剂量，需要将22.4 mg/kg 乘以小鼠的K 系数（3），再除以大鼠的K 系数（6），得到白藜芦醇用于大鼠的等效剂量为11.2 mg/kg 。
AZD3965_CAS号1448671-31-5说明书_AbMole中国
Activity of the monocarboxylate transporter 1 inhibitor AZD3965 in small cell lung cancer. Polański R, et al. Clin Cancer Res. 2014 Feb 15;20(4):926-37. PMID: 24277449.
mg/kg
换算成大鼠的剂量，需要将22.4
mg/kg
乘以小鼠的Km系数（3），再除以大鼠的Km系数
参考文献
Inhibition of monocarboxylate transporter-1 (MCT1) by AZD3965 enhances radiosensitivity by reducing lactate transport. Bola BM, et al. Mol Cancer Ther. 2014 Dec;13(12):2805-16. PMID: 25281618.
不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）
小鼠
大鼠
兔
豚鼠
仓鼠
狗
重量 (kg)
0.08
10
体表面积 (m2)
0.007
0.025
0.15
0.05
0.02
0.5
Km 系数
3
6
12
8
5
20
动例物如，A依(m据g/体kg表) =面动积物折算B (法m，g/k将g白) ×藜动动芦物物醇BA用的的于KK小mm系系鼠数数的剂量22.4 （6），得到白藜芦醇用于大鼠的等效剂量为11.2 。 mg/kg
AZD3965 目录号M5189
化学数据
分子量 分子式 号 CAS 储存条件
PCI-32765 (Ibrutinib)_Bruton's tyrosine kinase (BTK)抑制剂_936563-96-1_Apexbio
特别声明
产品仅用于研究， 不针对患者销售，望谅解。 每个产品具体的储存和使用信息显示在产品说明书中。ApexBio 产品在推荐的条件下是稳定 的。产品会根据不同的推荐温度进行运输。许多产品短期运输是稳定的，运输温度不同于长 期储存的温度。我们确保我们的产品是在保持试剂质量的条件下运输的。收到产品后，按照 产品说明书上的要求进行储存。
PCI-32765,Ibrutinib,CRA-0327 65
2-[(2R)-2-methylpyrrolidin-2-yl]-1H-benzimidazole-4-carboxamide
C=CC(=O)N1CCCC(C1)N2C3=C(C(=N2)C4=CC=C(C=C4)OC5=CC=CC=C 5)C(=NC=N3)N
引用文献
1. Schroeder JT, Bieneman AP. "Activation of Human Basophils by A549 Lung Epithelial Cells Reveals a Novel IgE-Dependent Response Independent of Allergen." J Immunol. 2017 Aug 1;199(3):855-865. PMID:28652400 2. Kosowicz JG, Lee J, et al. "Drug modulators of B cell signaling pathways and Epstein-Barr virus lytic activation." J Virol. 2017 May 31. pii: JVI.00747-17. PMID:28566383 3.Lee DD, Muskaj I, et al. "Platelet proteins cause basophil histamine release through an immunoglobulin-dependent mechanism. Transfusion." 2017 May 4. PMID:28470742
Etomoxir_CAS号124083-20-1_M9048说明书_AbMole中国
分子量326.82溶解性（25°C）DMSO ≥ 40 mg/mL分子式C17H23ClO4WaterCAS号124083-20-1Ethanol储存条件3年 -20°C 粉末状生物活性Etomoxir 是一种有效的肉毒碱棕榈酰基转移酶 (CPT-1) 抑制剂。
Etomoxir不可逆地结合CPT-1的催化位点抑制其活性，但也上调脂肪酸氧化酶。
肝脏中的Etomoxir可以作为过氧化物酶体增殖剂，增加DNA合成和肝脏生长。
因此，除了作为CPT1抑制剂外，etomoxir可被认为是PPARα激动剂。
在体内研究中，每天给大鼠注射Etomoxir，以20 mg/kg体重注射8天。
经Etomoxir处理的大鼠心脏CPT-I活性降低44%。
用20 mg/kg Etomoxir处理Lewis大鼠8天不会改变血糖。
不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）小鼠大鼠兔豚鼠仓鼠狗重量 (kg)0.020.15 1.80.40.0810体表面积 (m)0.0070.0250.150.050.020.5K系数36128520动物 A (mg/kg) = 动物 B (mg/kg) ×动物 B的K系数动物 A的K系数例如，依据体表面积折算法，将白藜芦醇用于小鼠的剂量22.4 mg/kg 换算成大鼠的剂量，需要将22.4 mg/kg 乘以小鼠的K系数（3），再除以大鼠的K系数（6），得到白藜芦醇用于大鼠的等效剂量为11.2 mg/kg。
参考文献FFA-ROS-P53-mediated mitochondrial apoptosis contributes to reduction of osteoblastogenesis and bone mass in type 2 diabetes mellitus.Li J, et al. Sci Rep. 2015 Jul 31;5:12724. PMID: 26226833.Etomoxir-induced partial carnitine palmitoyltransferase-I (CPT-I) inhibition in vivo does not alter cardiac long-chain fatty acid uptake and oxidation rates.Luiken JJ, et al. Biochem J. 2009 Apr 15;419(2):447-55. PMID: 19138173.Etomoxir 目录号M9048化学数据2mmmm m。
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分子量567.01
溶解性（25°C）DMSO分子式CHFNO.HClWater <1 mg/mL
CAS号8173837-23-1Ethanol <1 mg/mL
储存条件3年 -20°C 粉末状
生物活性
AC480 (BMS-599626)是一种选择性的，高效效的HER1和HER2抑制剂，IC50分别为20 nM和30 nM。比对HER4效果强8倍左右，而比对VEGFR2， c-Kit， Lck，
MET等的作用强100倍以上。BMS-599626选择性抑制重组HER1和HER2激酶的酶活性， IC50 分别为20 nM和 30 nM。 此外, BMS-599626也抑制相关受体HER4, 但
是抑制效果低点(IC50为190 nM)。BMS-599626定义为HER1的ATP竞争性抑制剂，HER2的ATP非竞争性抑制剂，K 分别为 2 nM 和 5 nM。
实验操作
来自于公开的文献，仅供参考
细胞实验
细胞系Sal2 mouse salivary gland tumor cells, .KPL-4 cells and PC9 cells
方法Cell assay. All cell lines were maintained in RPMI 1640 supplemented with 10% fetal bovine serum, 100 units/mL penicillin, and 100
Ag/mL streptomycin. Cells were plated at 1,000 per well in 96-well plates and were cultured for 24 hours before test compounds were
added.Compounds were diluted in culture medium such that the final concentration of DMSO never exceeded 1%.Following the
addition of compounds, the cells were cultured for an additional 72 hours before cell viability was determined by measuring the
conversion of 3-(4,5-dimethylthiazol- 2-yl)-2,5-diphenyltetrazolium bromide dye with the CellTiter96 kit (Promega, Madison, WI).
浓度0~10µM
处理时间72 h
动物实验
动物模型SAL2 murine salivary gland tumor, mice bearing KPL-4 human breast tumors and GEO human colon tumor models
配制dissolved in a mixture of propylene glycol/water (50:50)
剂量SAL2: 60, 120, 240 mg/kg daily for 14 days(d10-24); GEO human colon tumors：120,180mg/ kg daily for 14 days(d10-24);mice
bearing KPL-4 human breast tumors: once daily for 21days) at 60 mg/kg and 180 mg/kg
给药处理oral
不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）
小鼠大鼠兔豚鼠仓鼠狗
重量 (kg)0.020.151.80.40.0810
体表面积 (m)0.0070.0250.150.050.020.5
K 系数36128520
动物 A (mg/kg) = 动物 B (mg/kg) ×
动物 B的K系数
动物 A的K系数
例如，依据体表面积折算法，将白藜芦醇用于小鼠的剂量22.4 mg/kg 换算成大鼠的剂量，需要将22.4 mg/kg 乘以小鼠的K系数（3），再除以大鼠的K系数
（6），得到白藜芦醇用于大鼠的等效剂量为11.2 mg/kg。
参考文献
BMS-599626
目录号M1684
化学数据
272783
i
2
m
m
m
mm
Phase I safety, pharmacokinetic and pharmacodynamic trial of BMS-599626 (AC480), an oral pan-HER receptor tyrosine kinase inhibitor, in patients with
advanced solid tumors.
Soria et al. Ann Oncol. 2012 Feb;23(2):463-71. PMID: 21576284.
AC480, formerly BMS-599626, a pan Her inhibitor, enhances radiosensitivity and radioresponse of head and neck squamous cell carcinoma cells in vitro and in
vivo.
Torres et al. Invest New Drugs. 2011 Aug;29(4):554-61. PMID: 20119866.
Discovery and preclinical evaluation of [4-[[1-(3-fluorophenyl)methyl]-1H-indazol-5-ylamino]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]carbamic acid, (3S)-3-
morpholinylmethyl ester (BMS-599626), a selective and orally efficacious inhibitor of human epidermal growth factor receptor 1 and 2 kinases.
Gavai et al. J Med Chem. 2009 Nov 12;52(21):6527-30. PMID: 19821562.
Preclinical antitumor activity of BMS-599626, a pan-HER kinase inhibitor that inhibits HER1/HER2 homodimer and heterodimer signaling.
Wong et al. Clin Cancer Res. 2006 Oct 15;12(20 Pt 1):6186-93. PMID: 17062696.