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Brigatinib

Brigatinib

CAS: 1197953-54-0

Molecular Formula: C29H39ClN7O2P

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Brigatinib - Names and Identifiers

Name Brigatinib
Synonyms 140455
brigatib
Brigatinib
Bogtinib (AP26113)
Brigatinib, AP26113
AP26113 (Brigatinib)
5-Chloro-N4-[2-(dimethylphosphinyl)phenyl]-N2-[2-methoxy-4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl]-2,4-pyrimidinediamine
5-chloro-N4-(2-(dimethylphosphoryl)phenyl)-N2-(2-methoxy-4-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)phenyl)pyrimidine-2,4-diamine
CAS 1197953-54-0
EINECS 1592732-453-0

Brigatinib - Physico-chemical Properties

Molecular FormulaC29H39ClN7O2P
Molar Mass584.0924
Density1.31±0.1 g/cm3(Predicted)
Boling Point781.8±70.0 °C(Predicted)
Solubility 10 mM in Ethanol
pKa8.14±0.42(Predicted)
Storage Condition-20℃
UseAs 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.

Brigatinib - Preparation solution concentration reference

 1mg5mg10mg
1 mM1.712 ml8.56 ml17.121 ml
5 mM0.342 ml1.712 ml3.424 ml
10 mM0.171 ml0.856 ml1.712 ml
5 mM0.034 ml0.171 ml0.342 ml
Last Update:2024-01-02 23:10:35

Brigatinib - Introduction

Target
Target Value
ALK
(Cell-free assay)
0.37 nM
ROS1
(Cell-free assay)
1.9 nM
FLT3
(Cell-free assay)
2.1 nM
IGF1R
(Cell-free assay)
24.9 nM
EGFR(C797S/del19)
(cell-based)
39.9 nM
Last Update:2024-04-10 22:29:15

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
Brigatinib
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Shanghai Macklin Biochemical Co., Ltd
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CAS: 1197953-54-0
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Shanghai Yuanye Bio-Technology Co., Ltd.
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CAS: 1197953-54-0
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409 Click to send a QQ message
Shanghai Macklin Biochemical Co., Ltd
Featured ProductsSpot supply
Product Name: Brigatinib (AP26113) Visit Supplier Webpage Request for quotation
CAS: 1197953-54-0
Tel: +86-18821248368
Email: Int06@meryer.com
Mobile: +86-18821248368
QQ: 495145328 Click to send a QQ message
WhatsApp: +86-18821248368
Shanghai Amole Biotechnology Co., Ltd.
Spot supply
Product Name: Brigatinib Request for quotation
CAS: 1197953-54-0
Tel: 400-968-2212
Email: 3623107365@qq.com
Mobile: 18916960931
QQ: 3623107365 Click to send a QQ message
Wechat: 18916960931
SHANGHAI ACMEC BIOCHEMICAL TECHNOLOGY CO., LTD.
Spot supply
Product Name: Brigatinib Visit Supplier Webpage Request for quotation
CAS: 1197953-54-0
Tel: +86-400-900-4166
Email: product@acmec-e.com
Mobile: +86-18621343501
QQ: 2881950922 Click to send a QQ message
Wechat: 18621343501
WhatsApp: +86-18621343501
MedChemExpress (MCE)
Multiple SpecificationsSpot supply
Product Name: AP-26113 Visit Supplier Webpage Request for quotation
CAS: 1197953-54-0
Tel: 609-228-6898
Email: sales@medchemexpress.com
     tech@medchemexpress.com
Mobile: 609-228-6898
BOC Sciences
Spot supply
Product Name: Brigatinib Visit Supplier Webpage Request for quotation
CAS: 1197953-54-0
Tel: +16314854226
Email: info@bocsci.com
Mobile: +16314854226
Linkedin: https://www.linkedin.com/company/boc-sciences
Product List: View Catalog
SKYRUN INDUSTRIAL CO.,LTD
Spot supply
Product Name: Brigatinib Visit Supplier Webpage Request for quotation
CAS: 1197953-54-0
Tel: +86 0571-86722205
Email: sales@chinaskyrun.com
Mobile: +8618958170122
QQ: 2531159185 Click to send a QQ messageSend QQ message
Wechat: chinaskyrun
Shanghai Yuanye Bio-Technology Co., Ltd.
Spot supply
Product Name: Brigatinib Visit Supplier Webpage Request for quotation
CAS: 1197953-54-0
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409 Click to send a QQ message
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Brigatinib
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