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Products are for research use only. Not for human use. We do not sell to patients.

Signaling Pathway

NVP-TAE 684

HY-10192

(TAE684; NVP TAE684)

NVP-TAE 684

NVP-TAE 684 Chemical Structure

NVP-TAE684(TAE684) is a highly potent and selective small-molecule ALK inhibitor, which blocked the growth of ALCL-derived and ALK-dependent cell lines with IC50 values between 2 and 10 nM.

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10 mM * 1 mL in DMSO $108 In-stock
5 mg $80 In-stock
10 mg $120 In-stock
50 mg $320 In-stock
100 mg $450 In-stock
200 mg Get quote
500 mg Get quote
Size Price Stock Quantity
Free sample   Apply now  
10 mM * 1 mL in DMSO €106 In-stock
5 mg €78 In-stock
10 mg €118 In-stock
50 mg €314 In-stock
100 mg €441 In-stock
200 mg Get quote
500 mg Get quote

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Product name: NVP-TAE 684
Cat. No.: HY-10192

NVP-TAE 684 Data Sheet

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    Purity: 99.83%

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Biological Activity of NVP-TAE 684

NVP-TAE684(TAE684) is a highly potent and selective small-molecule ALK inhibitor, which blocked the growth of ALCL-derived and ALK-dependent cell lines with IC50 values between 2 and 10 nM.
IC50 value: 2-10 nM [1]
Target: ALK
in vitro: TAE684 does not exhibit significant cross-reactivity against other kinases. TAE684 potently inhibits the proliferation of Ba/F3 NPM-ALK cells with IC50 of 3 nM, without affecting the survival of Ba/F3 cells even at 1 μM. TAE684 also inhibits proliferation of NPM-ALK-expressing human ALCL cell lines including Karpas-299 and SU-DHL-1 with IC50 of 2–5 nM. Molecular modeling reveals that L258 may be one of the major kinase-selectivity determinants for TAE684. TAE684 treatment results in a rapid and sustained inhibition of phosphorylation of NPM-ALK. TAE684 induces apoptosis and G1 phase arrest in NPM-ALK-expressing Ba/F3 cells and ALCL patient cell lines [1]. TAE684 markedly overcomes Crizotinib-resistance in H3122 CR cells, harboring the fusion oncogene EML4-ALK, decreasing cell growth, suppressing ALK phosphorylation and inducing apoptosis [2]. Neurite outgrowth induced by expression of the mALK R1279Q mutant could be completely inhibited by TAE684 at 30 nM [3].
in vivo: After 4 weeks of treatment with TAE684 at 3 and 10 mg/kg, there is a significant delay in lymphoma development and 100- to 1,000-fold reduction in luminescence signal, without any signs of compound- or disease-related toxicity in Karpas-299 lymphoma model. TAE684 treatment also induces disease regression in established Karpas-299 lymphomas and down-regulates CD30 expression [1]. TAE684 also shows impressive antitumor activity against H3122 CR xenograft tumors [2]. treatment with TAE684 improves the rough eye phenotype of both ALK mutants, especially that seen with ALKR1275Q, whereas Crizotinib has little effect on either phenotype [3].

Protocol (Extracted from published papers and Only for reference)

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Chemical Information

M.Wt 614.2 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C30H40ClN7O3S
CAS No 761439-42-3
Solvent & Solubility

DMSO ≥28mg/mL Water <1.2mg/mL Ethanol ≥1.8mg/mL

Preparing Stock Solutions

1 mg 5 mg 10 mg
1 mM 1.6281 mL 8.1407 mL 16.2813 mL
5 mM 0.3256 mL 1.6281 mL 3.2563 mL
10 mM 0.1628 mL 0.8141 mL 1.6281 mL

References on NVP-TAE 684

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