CAS |
1197953-54-0 |
Chinese Name |
布格替尼 |
English Name |
Brigatinib |
Synonym |
;Brigatinib;Ap26113,brigatinib;AP26113;AP-26113; |
Unit |
Bottle |
Purity |
≥98% |
Molecular Formula |
C29H39ClN7O2P |
Molecular Weight |
584.09 |
Appearance |
White to yellow solid |
Storage |
Powder : -20℃, 2 years |
Solubility |
Soluble in DMSO≥ 0.1mg/ml |
EC |
EINECS 1592732-453-0 |
MDL |
MFCD29472221 |
InChIKey |
AILRADAXUVEEIR-UHFFFAOYSA-N |
InChI |
InChI=1S/C29H39ClN7O2P/c1-35-15-17-37(18-16-35)21-11-13-36(14-12-21)22-9-10-24(26(19-22)39-2)33-29-31-20-23(30)28(34-29)32-25-7-5-6-8-27(25)40(3,4)38/h5-10,19-21H,11-18H2,1-4H3,(H2,31,32,33,34) |
PubChem CID |
68165256 |
SMILES |
CN1CCN(CC1)C2CCN(CC2)C3=CC(=C(C=C3)NC4=NC=C(C(=N4)NC5=CC=CC=C5P(=O)(C)C)Cl)OC |
Description |
It is a potent and selective ALK inhibitor. |
Target Point |
ALK;EGFR;FLT3;IGF-1R;ROS1 |
Passage |
Angiogenesis; Protein Tyrosine Kinase/RTK |
IC50 |
0.6 nM (ALK)[1] |
Data Literature Source |
[1]. Zhang S, et al. The Potent ALK Inhibitor Brigatinib (AP26113) Overcomes Mechanisms of Resistance to First- and Second-Generation ALK Inhibitors in Preclinical Models. Clin Cancer Res. 2016 Nov 15;22(22):5527-5538
[2]. Huang WS, et al. Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase. J Med Chem. 2016 May 26;59(10):4948-64.
[3]. Siaw JT, et al. Brigatinib, an anaplastic lymphoma kinase inhibitor, abrogates activity and growth in ALK-positive neuroblastoma cells, Drosophila and mice. Oncotarget. 2016 May 17;7(20):29011-22 |
Specification |
5mg 10mg 50mg 100mg |