Bioactivity | NVP-TAE 684 (TAE 684) is a highly potent and selective ALK inhibitor, which blocks the growth of ALCL-derived and ALK-dependent cell lines with IC50 values between 2 and 10 nM[1]. | ||||||||||||
Invitro | TAE684 inhibits the proliferation of Ba/F3 NPM-ALK cells with an IC50 of 3 nM, without affecting the survival of parental Ba/F3 cells at concentrations up to 1 μM. TAE684 inhibits STAT3 and STAT5 phosphorylation in a dose-dependent manner in both Ba/F3 NPM-ALK and Karpas-299 cells. TAE684 induces apoptosis and G1 phase arrest in NPM-ALK-expressing Ba/F3 cells and ALCL patient cell lines[1]. NVP-TAE684 markedly reduces cell survival in both sensitive H3122 and H3122 CR cells, but has little to no effect on the viability of other, non-ALK-dependent cancer cell lines. NVP-TAE684 treatment of H3122 CR cells suppresses phosphorylation of ALK, AKT, and ERK and induces marked apoptosis. TAE684 potently suppresses the survival of Ba/F3 cells expressing the EML4-ALK L1196M mutant[2]. Neurite outgrowth induced by expression of the mALKR1279Q mutant is completely inhibited at 30 nM NVP-TAE684, which is comparable with the response seen with activated wt mALK[3]. | ||||||||||||
Name | NVP-TAE 684 | ||||||||||||
CAS | 761439-42-3 | ||||||||||||
Formula | C30H40ClN7O3S | ||||||||||||
Molar Mass | 614.20 | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
|