Lapatinib-d4 (tosylate)
目录号 : GC40222
An internal standard for the quantification of lapatinib
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Lapatinib-d4 is intended for use as an internal standard for the quantification of lapatinib by GC- or LC-MS. Lapatinib is a dual inhibitor of the EGF receptor (EGFR) and ErbB2 (IC50s = 19 and 3 nM, respectively). It inhibits the growth of EGFR-overexpressing A431 skin cancer and ErbB2-overexpressing SK-BR-3 breast cancer cells (IC50s = 0.14 and 0.124 μM, respectively). Lapatinib also inhibits the growth of ErbB2-amplified OD19 esophageal and NCI-N87 gastric cancer cells (IC50s = 0.09 and 0.01 μM, respectively) as well as several types of gastric cancer cells in which ErbB2 is not amplified (IC50s = 0.35-8.58 μM). It induces apoptosis in NCI-N87 and OD19 cells when used at a concentration of 1 μM. Lapatinib (50 mg/kg) reduces tumor growth in a BT474 breast cancer mouse xenograft model. It also reduces tumor growth in an NCI-N87 mouse xenograft model when administered at a dose of 100 mg/kg and induces tumor regression when used in combination with trastuzumab. Formulations containing lapatinib have been used in combination with other therapeutics in the treatment of ErbB2/HER2-overexpressing breast cancer.
| Cas No. | SDF | ||
| 分子式 | C29H22ClD4FN4O4S • 2C7H8O3S | 分子量 | 929.5 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| General tips | 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；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.0758 mL | 5.3792 mL | 10.7585 mL |
| 5 mM | 0.2152 mL | 1.0758 mL | 2.1517 mL |
| 10 mM | 0.1076 mL | 0.5379 mL | 1.0758 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Efficacy and safety of remimazolam tosylate in hysteroscopy: A randomized, single-blind, parallel controlled trial
J Clin Pharm Ther 2022 Jan;47(1):55-60.PMID:34655087DOI:10.1111/jcpt.13525.
What is known and objective: To compare the effectiveness and safety of remimazolam tosylate and propofol for hysteroscopy. Methods: From November 2020 to June 2021, a total of 90 patients who underwent hysteroscopy were prospectively enrolled in this study. The patients were randomly assigned to three groups: propofol group (group A), low-dose remimazolam tosylate group (group B), and high-dose remimazolam tosylate group (group C), with 30 cases in each group. All cases received intravenous sufentanil 0.1ug/kg for analgesic preconditioning. Patients in group A were given 2 mg/kg propofol intravenously, and maintained at a rate of 5 mg/kg/h. Patients in groups B and C were given intravenous remimazolam tosylate 0.25 mg/kg. Group B was maintained with remimazolam tosylate at a rate of 0.48 mg/kg/h, while group C was at a rate of 0.6 mg/kg/h. The changes of heart rate (HR), mean arterial pressure (MAP) and saturation of peripheral oxygen (SpO2) were recorded after admission (T0), 1 min after anaesthesia (T1), dilation of the uterine cavity (T2), and the end of hysteroscopy (T3). In addition, Observer's Assessment of Alertness/Sedation Scale (OAA/S) at 1 min, 3 min, and 5 min after hysteroscopy, the incidence of adverse events, and the time from the end of the hysteroscopy to reach the discharge standard, were recorded. Results and discussion: The success rate of sedation in each group was 100%. After administration, the adverse event incidence in group A was significantly higher than that in groups B and C (p < 0.05, respectively). Compared with propofol, remimazolam tosylate did not cause injection pain, had less impact on haemodynamics and caused less respiratory depression. What is new and conclusion: Remimazolam tosylate and propofol have similar success rates for painless hysteroscopy, and both can provide safe and effective sedation. The safety of remimazolam tosylate for hysteroscopy appears to be better than that of propofol.
Edoxaban tosylate
Am J Cardiovasc Drugs 2011;11(2):129-35.PMID:21446778DOI:10.2165/11533660-000000000-00000.
Daiichi Sankyo is developing edoxaban tosylate (DU 176b; DU-176; DU-176b; DU176b) as an orally active direct factor Xa inhibitor for the prevention of stroke and the prevention and treatment of venous thromboembolism. Two dosing regimens of edoxaban tosylate are being compared with warfarin over 24 months in the ENGAGE AF TIMI 48 trial (NCT00781391) in over 21 000 patients with atrial fibrillation in North and South America, Africa, Asia, Europe, Australia, and New Zealand. Edoxaban tosylate is also being compared with warfarin in the treatment and prevention of recurrent thromboembolic events in approximately 7500 patients with deep-vein thrombosis and/or pulmonary embolism in the HOKUSAI VTE trial (NCT00986154) being conducted in 40 countries. This review discusses the development history and scientific profile of this new compound.
Glycopyrronium tosylate (Qbrexza) for Hyperhidrosis
Skin Therapy Lett 2019 Mar;24(2):1-3.PMID:30970203doi
Hyperhidrosis is a condition characterized by excessive sweat production beyond which is physiologically necessary for thermal regulation. Affecting over 4.8% of the United States population, studies have shown that severe primary hyperhidrosis interferes with daily activities and can be considered intolerable, negatively impacting a patient’s quality of life. Glycopyrronium tosylate is a topical anticholinergic agent that reduces sweat production by blocking the activation of acetylcholine receptors in peripheral sweat glands. In clinical trials, topical glycopyrronium tosylate, a pre-moistened cloth containing 2.4% glycopyrronium solution, was shown to be an effective, safe and non-invasive treatment for patients suffering from primary hyperhidrosis. This review examines the clinical trials of topical glycopyrronium tosylate and its role in primary hyperhidrosis. Glycopyrronium tosylate was recently US FDA-approved (as of June 2018) to manage patients with primary axillary hyperhidrosis.
tosylate salts of the anticancer drug lapatinib
Acta Crystallogr C 2013 Dec 15;69(Pt 12):1516-23.PMID:24311503DOI:10.1107/S0108270113028965.
Two tosylate salts of an anticancer drug lapatinib, viz. a monotosylate [systematic name: ({5-[4-({3-chloro-4-[(3-fluorophenyl)methoxy]phenyl}amino)quinazolin-6-yl]furan-2-yl}methyl)[2-(methylsulfonyl)ethyl]azanium 4-methylbenzenesulfonate], C29H27ClFN4O4S(+)·C7H7O3S(-), (I), and a ditosylate [systematic name: 4-({3-chloro-4-[(3-fluorophenyl)methoxy]phenyl}amino)-6-]5-({[2-(methylsulfonyl)ethyl]azaniumyl}methyl)furan-2-yl[quinazolin-1-ium bis(4-methylbenzenesulfonate)], C29H28ClFN4O4S(2+)·2C7H7O3S(-), (II), were obtained during crystallization attempts for polymorphism. In both structures, the lapatinib cation is in a distorted U-like conformation and the tosylate anion is clamped between the aniline N atom and methylamine N atom through N-H···O hydrogen bonds, forming an R2(2)(15) ring motif. The 4-anilinoquinazoline ring system is essentially planar in (I), while it is twisted in (II), controlled by an intramolecular C-H···N interaction. In (I), alternating cations and anions are linked by N-H···O hydrogen bonds into C2(2)(6) chains. These chains are linked by cations in a helical manner. The presence of the additional tosylate anion in (II) results in the formation of one-dimensional tapes of fused hydrogen-bonded rings through N-H···O and C-H···O interactions. These studies augment our understanding of the role of nonbonded interactions in the solid state, which is useful for correlation to the physicochemical properties of drug products.
The Choice of Anesthetic Drugs in Outpatient Hysteroscopic Surgery: A Systematic Review and Network Meta-Analysis
Dis Markers 2022 Sep 21;2022:2408685.PMID:36188426DOI:10.1155/2022/2408685.
Objective: Hysteroscopy is a minimally invasive gynecologic technique that is widely practiced in outpatient procedures. The choice of anesthesia is a key factor for the surgical outcome and postoperative recovery. This study was conducted to assess the effects of different anesthetic modalities based on dexmedetomidine in outpatient hysteroscopic surgery anesthesia. Methods: We did a systematic review and network meta-analysis of outpatient hysteroscopic surgery anesthesia. We searched Pubmed, Embase, and Cochrane-Library from database inception to December 31, 2021. Duplicate literature was excluded and screened separately for initial screening at three tiers: article title, abstract, and full text before deciding whether to include in this study against the above criteria. Results after analysis of categorical variables were expressed as ORR Ratio (95% CI) and continuous variables were expressed as Mean Difference (95% CI). Data collation and analyses were performed using the gemtc package in the R language. Results: Four trials were finally included with data for 301 participants, three anesthetic drugs, and five anesthetic modalities. A fixed-effects model was used for the different anesthesia modalities without significant heterogeneity (all I2<20%) in the analysis of adverse events (AEs), the incidence of respiratory depression, operative time, and time in the post-anesthesia care unit (PACU). Remimazolam tosylate was associated with a lower incidence of AEs versus dexmedetomidine, and significant differences between dexmedetomidine and propofol were absent. Propofol and various doses of remimazolam tosylate resulted in a lower incidence of respiratory depression versus dexmedetomidine, with an absence of differences between propofol and dexmedetomidine. The operative time for different anesthetic modalities was, in descending order, dexmedetomidine < remimazolam tosylate (0.60 mg/kg/h <0.48 mg/kg/h) < propofol < remimazolam tosylate (1.00 mg/kg/h), despite the absence of intergroup differences. Propofol was associated with a longer time in PACU versus dexmedetomidine and remimazolam tosylate (1.00 mg/kg/h); those of dexmedetomidine and remimazolam tosylate (1.00 mg/kg/h) were similar. The time in PACU for different anesthetic modalities, in descending order, was dexmedetomidine < remimazolam tosylate (1.00 mg/kg/h) < propofol. Propofol was associated with a longer time in PACU versus dexmedetomidine and remimazolam tosylate. Conclusion: In outpatient hysteroscopic surgery anesthesia, dexmedetomidine was associated with a higher incidence of AEs and respiratory depression and a shorter operative time and time in PACU versus remimazolam tosylate and propofol. Remimazolam tosylate showed safety benefits with a similar duration of PACU stay versus dexmedetomidine. Therefore, the choice of anesthetic drugs in outpatient surgery requires consideration of the patient's conditions and preferences.