Tucatinib (Irbinitinib)
(Synonyms: 妥卡替尼,Irbinitinib; ARRY-380; ONT-380) 目录号 : GC32726
An inhibitor of HER2
Cas No.:937263-43-9
Sample solution is provided at 25 µL, 10mM.
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Tucatinib is an inhibitor of HER2 (IC50 = 14 nM).1 It inhibits the phosphorylation of HER2 in BT474 breast carcinoma cells (IC50 = 21 nM). Tucatinib inhibits phosphorylation of AKT and induces apoptosis in BT474 cells. In vivo, tucatinib (25-100 mg/kg) inhibits tumor growth in NCI N87 gastric carcinoma and SKOV3 ovarian adenocarcinoma mouse xenograft models. Tucatinib also reduces intratumor phosphorylation of AKT and ERK and inhibits tumor growth in a BT474 mouse xenograft model.
1.Pheneger, T., Bouhana, K., Anderson, D., et al.Abstract #1795: In vitro and in vivo activity of ARRY-380: A potent, small molecule inhibitor of ErbB2AACR Cancer Res.69(9)1795(2009)
Animal experiment: | Mice: For the SKOV-3 tumor studies, female nude mice are inoculated with cells subcutaneously in the flank. Animals received: doses of Tucatinib ranging up to 200 mg/kg/d, PO; and/or Trastuzumab at 20 mg/kg, IP, Q3D or QW; and/or RP-56976 at 10 mg/kg, IV, Q3D; and/or Bevacizumab at 10 mg/kg, IP, Q4D x3. Tumor size is measured at regular intervals and subsets of animals are monitored for up to 90 days to determine tumor-free survival[3]. |
References: [1]. Moulder-Thompson S, et al. Phase 1 Study of ONT-380, a HER2 Inhibitor, in Patients with HER2+ Advanced Solid Tumors, with an Expansion Cohort in HER2+ Metastatic Breast Cancer (MBC). Clin Cancer Res. 2017 Jan 4. pii: clincanres.1496.2016. | |
| Cas No. | 937263-43-9 | SDF | |
| 别名 | 妥卡替尼,Irbinitinib; ARRY-380; ONT-380 | ||
| Canonical SMILES | CC1=CC(NC2=C3C=C(NC4=NC(C)(C)CO4)C=CC3=NC=N2)=CC=C1OC5=CC6=NC=NN6C=C5 | ||
| 分子式 | C26H24N8O2 | 分子量 | 480.52 |
| 溶解度 | DMSO : 50 mg/mL (104.05 mM) | 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 | 2.0811 mL | 10.4054 mL | 20.8108 mL |
| 5 mM | 0.4162 mL | 2.0811 mL | 4.1622 mL |
| 10 mM | 0.2081 mL | 1.0405 mL | 2.0811 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。
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet