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NVP-TAE684 | ALK inhibitor

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Price:
$149.00
Catalog #:
C6823-5
Quantity:


Product Description

NVP-TAE684 is an aminopyrimidine-based, ATP-competitive inhibitor of ALK (IC50, 3 nM) with additional activity vs Flt3 and Tie2 at values of 3 nM, and 12 nM, respectively. Despite ALK's high sequence homology with insulin receptor kinase (InsR), cellular InsR potency of NVP-TAE684 in Ba/F3 Tel-Flt3 and Ba/F3 Tel-Tie2 cell lines was 554 nM and >1 uM, respectively. [1]

In human anaplastic large-cell lymphoma (ALCL) cell lines expressing NPM-ALK, NVP-TAE684 inhibits proliferation of Karpas-29 and SU-D HL-1 cell lines with an IC50 range of 2-5 nM. Additionally, NVP-TAE684 inhibits phosphorylation of downstream of both ERK and Akt in Karpas-299 cells, thus aiding in the confirmation that STAT, RAS/FAR/MAPK, and PI3K/Akt are activated by NPM-ALK in ALCL cell lines.

NVP-TAE684 has been shown to be efficacious in neuroblastoma lines with constitutively active ALK mutations (G1128A, I1171N, F1174L, R1192P, F1245C, R1275Q). [2] Additionally, NVP-TAE684 is effective in crizotinib-resistant EML4-ALK L1196M mutants as well as other secondary gatekeeper mutations. [2]


Technical information:

Chemical Formula:   C30H40ClN7O3S
CAS #:   761439-42-3
Molecular Weight:   614.2
Purity:   >98%
Appearance:   Pale Yellow
Chemical Name:   5-chloro-N4-(2-(isopropylsulfonyl)phenyl)-N2-(2-methoxy-4-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)phenyl)pyrimidine-2,4-diamine
Solubility:   Up to 15 mM in DMSO
Synonyms:   NVP-TAE684, TAE684, TAE-684

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.


Reference:

1. Galkin et al., Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. Proc. Natl. Acad. Sci. 2007, 104(1), 270-275. Pubmed ID: 17185414
2. Schonherr et al., Activating ALK mutations found in neuroblastoma are inhibited by Crizotinib and NVP-TAE684. Biochem. J. 2011, 440, 405-413. Pubmed ID: 21838707
3. Katayama et al., Therapeutic strategies to overcome crizotinib resistance in non-small cell lung cancers harboring the fusion oncogene EML4-ALK. Proc. Natl. Acad. Sci. 2011, 108(18), 7535-7540. Pubmed ID: 21502504

Other Information:

Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.

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