AP26113 (Brigatinib)
Brigatinib
CAS: 1197953-54-0
Molecular Formula: C29H39ClN7O2P
AP26113 (Brigatinib) - Names and Identifiers
AP26113 (Brigatinib) - Physico-chemical Properties
| Molecular Formula | C29H39ClN7O2P |
| Molar Mass | 584.0924 |
| Density | 1.31±0.1 g/cm3(Predicted) |
| Boling Point | 781.8±70.0 °C(Predicted) |
| Solubility | 10 mM in Ethanol |
| pKa | 8.14±0.42(Predicted) |
| Storage Condition | -20℃ |
| Use | As a new generation of tyrosine kinase inhibitor, bouglitinib has a significant effect on ALK + metastatic NSCLC, august 30, 2016 U. S. Food and Drug Administration (FDA) awarded bougatinib as breakthrough therapy for patients with progression or intolerance to crizotinib, a first-generation ALK + NSCLC treatment status, priority is given to the review of marketing applications and the treatment of allowing the rolling submission of application materials. The FDA approved the marketing of bouglitinib on 4/28/2017 under the trade name Alunbrigtm. |
AP26113 (Brigatinib) - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.712 ml | 8.56 ml | 17.121 ml |
| 5 mM | 0.342 ml | 1.712 ml | 3.424 ml |
| 10 mM | 0.171 ml | 0.856 ml | 1.712 ml |
| 5 mM | 0.034 ml | 0.171 ml | 0.342 ml |
Last Update：2024-01-02 23:10:35
AP26113 (Brigatinib) - Introduction
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Last Update：2024-04-10 22:29:15
AP26113 (Brigatinib) - Introduction
use
bugatinib is a tyrosine kinase receptor (MERTK) inhibitor that can be used in combination with epidermal growth factor receptor (EGFR) inhibitors in cancer treatment.
pharmacological action
bugatinib is a tyrosine kinase inhibitor. it has inhibitory activity on a variety of kinases, including ALK,ROS1 proto-oncogene (C-rosproto-oncogene1), insulin-like growth factor -1receptor (insulin-likegrowthfactor1receptor,IGF-1R), FMS-like tyrosine kinase 3(fms-liketyrosinekinase,FLT-3), epidermal growth factor receptor (EGFR) deletion and point mutation at concentrations that can be achieved in vitro and clinically. In vitro and in vivo tests, bugatinib inhibited the phosphorylation of ALK itself and ALK mediated the phosphorylation of the downstream signaling proteins STAT3,AKT,ERK1/2 and S6. Bugitinib also inhibited the proliferation of cell lines expressing EML4-ALK and NPM-ALK fusion proteins in vitro and showed a dose-related effect in mice to inhibit the growth of EML4-ALK NSCLC xenografts. Clinically, it can achieve a concentration of ≤ 500nmol • L-1, bugatinib inhibits the expression of EML4-ALK cells in vitro and the survival rate of 17 mutants, which are associated with resistance to ALK inhibitors, including crizotinib and EGFR-Del(E746-A750), ROS1-L2026M, FLT3-F691L and FLT3-D835Y. In vivo, bugatinib also showed antitumor activity against four EML4-ALK mutants, including G1202R and L1196M mutants isolated from plasma in NSCLC patients whose disease has progressed after treatment with crizotinib. Bugitinib can reduce the ALK load of intracranial implantation with driving tumor cell lines and prolong the survival of mice.
Last Update：2024-04-09 20:52:54
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Product Name: Brigatinib Visit Supplier Webpage Request for quotationCAS: 1197953-54-0
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Spot supply
Product Name: Brigatinib Visit Supplier Webpage Request for quotationCAS: 1197953-54-0
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Spot supply
Product Name: Brigatinib Visit Supplier Webpage Request for quotationCAS: 1197953-54-0
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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