Network Version
NVP-TAE 684 Data Sheet
| Product Name: | NVP-TAE 684 |
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|---|---|---|
| CAS No.: | 761439-42-3 | |
| Cat. No.: | HY-10192 | |
| MWt: | 614.2 | |
| Formula: | C30H40ClN7O3S | |
| Purity : | >98% | |
| Solubility: | DMSO : 7.69 mg/mL (12.52 mM; Need ultrasonic) | |
| Mechanisms: | Target: Cancer | |
| Biological Activity: | ||
| 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]. IC50 & Target: IC50: 2-10 nM (ALK-dependent cell lines)[1] In Vitro: 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]. In Vivo: NVP-TAE684 suppresses lymphomagenesis in two independent models of ALK-positive ALCL and induces regression of established Karpas-299 lymphomas. TAE684 displays appreciable bioavailability and half-life in vivo. TAE684 (1, 3, and 10 mg/kg. p.o.) significantly delays in lymphoma development and shows 100- to 1,000-fold reduction in luminescence signal. The TAE684- (10 mg/kg) treated group appeares healthy and does not display any signs of compound- or disease-related toxicity[1]. | ||
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