Copanlisib dihydrochloride
(Synonyms: 库潘尼西盐酸; BAY 80-6946 dihydrochloride) 目录号 : GC60112
A selective PI3K inhibitor
Cas No.:1402152-13-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Copanlisib is an inhibitor of class I phosphoinositide 3-kinase (PI3K) isoforms (IC50s = 0.5, 3.7, 6.4, and 0.7 nM for α, β, γ, and δ, respectively).1 It is weakly active or inactive against numerous other kinases. Copanlisib is effective in vivo when administered intravenously, inhibiting PI3K signaling and inducing tumor regression via apoptosis in xenograft tumors in mice.1,2
1.Liu, N., Rowley, B.R., Bull, C.O., et al.BAY 80-6946 is a highly selective intravenous PI3K inhibitor with potent p110α and p110δ activities in tumor cell lines and xenograft modelsMol. Cancer Ther.12(11)2319-2330(2013) 2.Will, M., Qin, A.C.R., Toy, W., et al.Rapid induction of apoptosis by PI3K inhibitors is dependent upon their transient inhibition of RAS-ERK signalingCancer Discov.4(3)334-347(2014)
| Cas No. | 1402152-13-9 | SDF | |
| 别名 | 库潘尼西盐酸; BAY 80-6946 dihydrochloride | ||
| Canonical SMILES | O=C(C1=CN=C(N)N=C1)NC2=NC3=C(OC)C(OCCCN4CCOCC4)=CC=C3C5=NCCN25.[H]Cl.[H]Cl | ||
| 分子式 | C23H30Cl2N8O4 | 分子量 | 553.44 |
| 溶解度 | 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 1.8069 mL | 9.0344 mL | 18.0688 mL |
| 5 mM | 0.3614 mL | 1.8069 mL | 3.6138 mL |
| 10 mM | 0.1807 mL | 0.9034 mL | 1.8069 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。
An industry update: the latest developments in therapeutic delivery
Ther Deliv 2018 Jan;9(1):9-15.PMID:29216806DOI:10.4155/tde-2017-0109
This industry update covers the period from 1 September through 30 September 2017, and is based on information sourced from company press releases, scientific literature, patents and various news websites. The month saw the US FDA approve three new molecular entities, Aliqopa (Copanlisib dihydrochloride) (Bayer Healthcare); Solosec (secnidazole) (Symbiomix Therapeutics) and Verzenio (abemaciclib) (Eli Lilly and Co). Intarcia Therapeutics Inc. has its application for approval of a novel drug device combination of exenatide for the treatment of diabetes rejected by FDA but said that it will work to address the concerns and refile the application. The impact of biosimilars in the market is steadily increasing with seven biosimilars approved in the USA and Sandoz hoping to add to this with its announcement that FDA has accepted its Biologics License Application for a biosimilar version of Roche's Rituxan. Circassia announced positive top line results of a respiratory drug, Duaklir (for the treatment of chronic obstructive pulmonary disease) and Sarepta (for its new treatment for Duchenne muscular dystrophy). Axovant Sciences Ltd announced the failure if its drug Intepirdine in the treatment of Alzheimer's, adding to a growing list of drug failures in this area. There were a number of developments in the area of oncology with Bristol-Myers Squibb and Infinity Pharmaceuticals announcing an expansion of their collaboration looking at combination treatments, as well as Eli Lilly and Co's approval for Verzenio. Rani Therapeutics and Intra-Cellular Therapies announced successful funding rounds to support their drug programs. Allergan announced a novel licensing deal for its dry eye drug, Restasis, which it hopes would allow it to stave off patent challenges from several companies looking to develop generic versions of the drug. New research suggests that loss of sense of smell can be linked to an increased risk of developing Parkinson's disease.