TAE684 Inhibitor CAS No. 761439-42-3

Cat. No.	Name	Size	Price
KI1270	TAE684	5 mg	$256
	TAE684	10 mg	$464
	TAE684	50 mg	$1232
	TAE684	200 mg	$2992

Chemical Characteristic

Product Name	TAE684
Synonyms	NVP-TAE684
CAS No.	761439-42-3
Molecular Weight	614.21
Formula	C₃₀H₄₀ClN₇O₃S
Chemical Name	5-chloro-2-N-[2-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl]-4-N-(2-propan-2-ylsulfonylphenyl)pyrimidine-2,4-diamine
Smiles	c1(nc(c(cn1)Cl)Nc1c(cccc1)S(=O)(=O)C(C)C)Nc1c(cc(cc1)N1CCC(CC1)N1CCN(CC1)C)OC
Chemical Structure

Biological activities

TAE684 is a potent ALK inhibitor with an IC50 of 3 nM. In vitro, TAE684 blocks proliferation and survival of Ba/F3 NPM-ALK, SU-DHL-1 and Karpas-299 cells with IC50 between 2 and 5 nM. TAE684 (10-500 nM) inhibits NPM-ALK and STAT3 activation in Ba/F3 NPM-ALK and Karpas-299 cells in a concentration- and time-dependent manner. TAE684 (50 nM) also induces cell cycle arrest and apoptosis in ALCL and Ba/F3 NPM-ALK cell lines.^[1] TAE684 (100 nM) markedly reduces cell survival in both sensitive H3122 and H3122 CR cells, but has little to no effect on the viability of non-ALK??ependent cancer cell lines (including A549, H1299, SKBR3, and H460). TAE684 treatment (30-300 nM) suppresses phosphorylation of ALK, AKT, and ERK and induces marked apoptosis in H3122 CR cells.^[2] In Karpas-299 tumor model, TAE684 treatment (10 mg/kg) inhibits NPM-ALK fusion kinase-mediated signaling and induces regression of established lymphomas.^[1] In H3122 xenograft model in vivo, TAE684 ( 10 and 25 mg/kg) effectively inhibits the tumor growth.^[3] In addition, TAE684 treatment (25 and 50 µM) improves the rough eye phenotype of both ALKF1174L and ALKR1275Q, especially that seen with ALKR1275Q, whereas crizotinib has little effect on either phenotype.^[4]

Protocols

In vitro: TAE684 is dissolved in DMSO.^[2]

References

[1] Galkin AV, et al. Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. Proc Natl Acad Sci U S A. 2007, 104(1): 270-275. [2] Katayama R, et al. Therapeutic strategies to overcome crizotinib resistance in non-small cell lung cancers harboring the fusion oncogene EML4-ALK. Proc Natl Acad Sci U S A. 2011, 108(18): 7535-7540 [3] Koivunen JP, et al. EML4-ALK fusion gene and efficacy of an ALK kinase inhibitor in lung cancer. Clin Cancer Res. 2008, 14(13): 4275-4283. [4] Schnherr C, et al. Activating ALK mutations found in neuroblastoma are inhibited by Crizotinib and NVP-TAE684. Biochem J. 2011, 440(3): 405-413.

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