CH7057288

InvivoChem Cat #:V4146CAS #:2095616-82-1Purity >=98%

Description: CH7057288 is a novel, potent and selective inhibitor of TRK (tyrosine receptor kinase) with IC50 values of 1.1 nM, 7.8 nM and 5.1 nM for TRKA, TRKB, and TRKC respectively. CH7057288 showed selective inhibitory activity against TRKA, TRKB, and TRKC in cell-free kinase assays and suppressed proliferation of TRK fusion-positive cell lines, but not that of TRK-negative cell lines. In subcutaneously implanted xenograft models of TRK fusion-positive cells, strong tumor growth inhibition was observed. Furthermore, CH7057288 induced regression of intracranial tumors and greatly improved event-free survival in an intracranial implantation model mimicking brain metastasis. Recently, resistant mutations in TRK have been reported in patients showing disease progression after treatment with a TRK inhibitor under clinical development. CH7057288 maintained similar levels of in vitro and in vivo activity against some of the resistant mutants as it did to wild-type TRK. In summary, CH7057288 could be a promising therapeutic agent for TRK fusion-positive cancer. TRK receptor tyrosine kinases are expressed as fusion proteins encoded by various fusion genes across a wide variety of cancer types, including lung and colorectal cancer. These fusion proteins have potent oncogenic activity and are thought to be an attractive therapeutic target.

Description:

References: http://cancerres.aacrjournals.org/content/77/13_Supplement/4179

References:

-20C for 3 years in powder form

Synonym: CH7057288; CH-7057288; CH 7057288
IUPAC/Chemical Name: N-(tert-butyl)-2-((6, 6-dimethyl-8-(methylsulfonamido)-11-oxo-6, 11-dihydronaphtho[2, 3-b]benzofuran-3-yl)ethynyl)-6-methylisonicotinamide
InChi Key: DCGOHGQJHJXBGW-UHFFFAOYSA-N
InChi Code: InChI=1S/C32H31N3O5S/c1-18-14-20(30(37)34-31(2, 3)4)16-21(33-18)10-8-19-9-12-24-26(15-19)40-29-27(24)28(36)23-13-11-22(35-41(7, 38)39)17-25(23)32(29, 5)6/h9, 11-17, 35H, 1-7H3, (H, 34, 37)
SMILES Code: CS(NC1=CC=C2C(C(C)(C)C(OC3=CC(C#CC4=NC(C)=CC(C(NC(C)(C)C)=O)=C4)=CC=C35)=C5C2=O)=C1)(=O)=O