Product Data?SheetLapatinibCat. No.:CAS No.:分?式:分?量:作?靶点:作?通路:储存?式:HY-50898231277-92-2C??H??ClFN?O?S581.06EGFR; Autophagy; FerroptosisJAK/STAT Signaling; Protein Tyrosine Kinase/RTK; Autophagy; ApoptosisPowderIn solvent-20°C4°C-80°C-20°C3 years2 years6 months1 monthInhibitors?Agonists?Screening Libraries溶解性数据体外实验DMSO : ≥ 39 mg/mL (67.12 mM)* \Mass1 mg5 mg10 mgSolventConcentration制备储备液1 mM5 mM10 mM1.7210 mL0.3442 mL0.1721 mL8.6050 mL1.7210 mL0.8605 mL17.2099 mL3.4420 mL1.7210 mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；?旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存?式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个?内使?，-20°C 储存时，请在 1 个?内使?。体内实验请根据您的实验动物和给药?式选择适当的溶解?案。以下溶解?案都请先按照 In Vitro ?式配制澄清的储备液，再依次添加助溶剂： 为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的?作液，建议您现?现配，当天使?； 以下溶剂前显?的百分?是指该溶剂在您配制终溶液中的体积占?；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的?式助溶1. 请依序添加每种溶剂：?10% DMSO ?? 40% PEG300 ?? 5% Tween-80 ?? 45% salineSolubility: ≥ 2.5 mg/mL (4.30 mM); Clear solution此?案可获得 ≥ 2.5 mg/mL (4.30 mM，饱和度未知) 的澄清溶液。 以 1 mL ?作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加? 50 μL Tween-80，混合均匀；然后继续加? 450 μL ?理盐?定容? 1 mL。2. 请依序添加每种溶剂：?10% DMSO ?? 90% corn oilSolubility: ≥ 2.5 mg/mL (4.30 mM); Clear solutionPage 1 of 2 www.MedChemExpress.cn
此?案可获得 ≥ 2.5 mg/mL (4.30 mM，饱和度未知) 的澄清溶液，此?案不适?于实验周期在半个?以上的实验。 以 1 mL ?作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL ??油中，混合均匀。BIOLOGICAL ACTIVITY?物活性Lapatinib (GW572016) 是?种 ErbB-2 和 EGFR 酪氨酸激酶结构域的有效抑制剂，对纯化的 EGFR 和 ErbB-2 的 IC50 值分别为 10.2 和 9.8 nM。IC?? & TargetEGFR10.2 nM (IC50, Cell Free Assay)体外研究Lapatinib (GW2016; 0.03-10 μM; 6 hours; BT474 and HN5 cells) treatment inhibits receptor autophosphorylation of EGFR and ErbB-2 in a dose-responsive manner. Phosphorylation of serine 473 of AKT was inhibited by GW2016 in a dose-dependent manner[1]. Lapatinib (GW2016; 72 hours; HN5, A-43, BT474, N87, and CaLu-3 cells) treatment has a selective inhibition of the proliferation of human tumor cell lines[1]. Lapatinib (GW2016; 1-10 μM; 72 hours; HN5 cells) treatment results in induces G1 arrest[1].Western Blot Analysis[1]Cell Line:Concentration:Incubation Time:Result:BT474 and HN5 cells0.03 μM, 0.1 μM, 0.3 μM, 1 μM, 3 μM, or 10 μM6 hoursInhibited receptor autophosphorylation of EGFR and ErbB-2 in a dose-responsive manner. Phosphorylation of serine 473 of AKT was also inhibited in a dose-dependent manner.Cell Proliferation Assay[1]Cell Line:Concentration:Incubation Time:Result:Cell Cycle Analysis[1]Cell Line:Concentration:Incubation Time:Result:HN5 cells1 μM, or 10 μM72 hoursResulted in induction of G1 arrest.72 hoursInhibited the growth of tumor cells overexpressing EGFR or ErbB-2.HN5, A-43, BT474, N87, and CaLu-3 cellsErbB29.8 nM (IC50, Cell Free Assay)体内研究Lapatinib (GW2016; 30-100 mg/kg; oral administration; twice daily; for 21 days; CD-1 nude female mice) treatment inhibits tumor xenograft growth of the HN5 cells in a dose-responsive manner at 30 and 100 mg/kg, with complete Page 2 of 3 www.MedChemExpress.cn
inhibition of tumor growth at the higher dose[1].Animal Model:Dosage:Administration:Result:CD-1 nude female mice (4-6 weeks old) with HN5 cells[1]30 mg/kg, 100 mg/kgOral administration; twice daily; for 21 daysInhibited tumor xenograft growth of the HN5 cells in a dose-responsive manner.客户使?本产品发表的科研?献????Nature. 2017 Aug 24;548(7668):471-475.????Nat Med. 2016 Jul;22(7):723-6.????Nat Immunol. 2024 Mar;19(3):233-245.????Sci Transl Med. 2024 Jul 18;10(450). pii: eaaq1093.????Oncogene. 2016 Jun 9;35(23):2961-70.See more customer validations on www.MedChemExpress.cnREFERENCES[1].?Rusnak DW, et al. The effects of the novel, reversible epidermal growth factor receptor/ErbB-2 tyrosine kinase inhibitor, GW2016, on the growth of human normal and tumor-derived cell lines in vitro and in vivo. Mol Cancer Ther. 2001 Dec;1(2):85-94McePdfHeightCaution: Product has not been fully validated for medical applications. For research use only.
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