Brigatinib-analog

Brigatinib-analog is an orally active, potent and selective anaplastic lymphoma kinase (ALK) and the epidermal growth factor receptor (EGFR) inhibitor. Brigatinib-analog is structurally related to Brigatinib (AP-26113). Brigatinib-analog binds to and inhibits ALK kinase and ALK fusion proteins as well as EGFR and mutant forms. This leads to the inhibition of ALK kinase and EGFR kinase, disrupts their signaling pathways and eventually inhibits tumor cell growth in susceptible tumor cells.

Product information

CAS Number: 1197958-12-5

Molecular Weight: 529.01

Formula: C26H34ClN6O2P

Synonym:

AP-26113-analog

AP26113-analog

AP 26113-analog

Chemical Name: (2-((5-chloro-2-((4-(4-(dimethylamino)piperidin-1-yl)-2-methoxyphenyl)amino)pyrimidin-4-yl)amino)phenyl)dimethylphosphine oxide

Smiles: CN(C)C1CCN(CC1)C1=CC(OC)=C(C=C1)NC1=NC(NC2=CC=CC=C2P(C)(C)=O)=C(Cl)C=N1

InChiKey: OVDSPTSBIQCAIN-UHFFFAOYSA-N

InChi: InChI=1S/C26H34ClN6O2P/c1-32(2)18-12-14-33(15-13-18)19-10-11-21(23(16-19)35-3)30-26-28-17-20(27)25(31-26)29-22-8-6-7-9-24(22)36(4,5)34/h6-11,16-18H,12-15H2,1-5H3,(H2,28,29,30,31)

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO, not in water

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

References:

1. Rossi A, Maione P, Sacco PC, Sgambato A, Casaluce F, Ferrara ML, Palazzolo G, Ciardiello F, Gridelli C. ALK inhibitors and advanced non-small cell lung cancer (review). Int J Oncol. 2014 Aug;45(2):499-508. doi: 10.3892/ijo.2014.2475. Epub 2014 May 29. PubMed PMID: 24889366.
2. Iwama E, Okamoto I, Harada T, Takayama K, Nakanishi Y. Development of anaplastic lymphoma kinase (ALK) inhibitors and molecular diagnosis in ALK rearrangement-positive lung cancer. Onco Targets Ther. 2014 Mar 5;7:375-85. doi: 10.2147/OTT.S38868. eCollection 2014. Review. PubMed PMID: 24623980; PubMed Central PMCID: PMC3949762.
3. Perez CA, Velez M, Raez LE, Santos ES. Overcoming the resistance to crizotinib in patients with non-small cell lung cancer harboring EML4/ALK translocation. Lung Cancer. 2014 May;84(2):110-5. doi: 10.1016/j.lungcan.2014.02.001. Epub 2014 Feb 8. PubMed PMID: 24598368.

Products are for research use only. Not for human use.