MLN8054 Inhibitor CAS No. 869363-13-3

Cat. No.	Name	Size	Price
KI1308	MLN8054	5 mg	$272
	MLN8054	10 mg	$512
	MLN8054	50 mg	$1552
	MLN8054	200 mg	$3952

Chemical Characteristic

Product Name	MLN8054
CAS No.	869363-13-3
Molecular Weight	476.86
Formula	C₂₅H₁₅ClF₂N₄O₂
Chemical Name	4-[[9-chloro-7-(2,6-difluorophenyl)-5H-pyrimido[5,4-d][2]benzazepin-2-yl]amino]benzoic acid
Smiles	C(=O)(c1ccc(cc1)Nc1nc2c(CN=C(c3c2ccc(c3)Cl)c2c(cccc2F)F)cn1)O
Chemical Structure

Biological activities

MLN8054 is a potent Aurora A inhibitor with an IC50 of 4 nM. MLN8054 is 40-fold more selective for Aurora A compared with the family member Aurora B and 100-fold selective for Aurora A compared with a panel of other kinases including PKC, CAMKII, CDK2E, and CDK1. In vitro, MLN8054 effectively inhibits the growth of colon tumor cell lines HCT-116, SW480, and DLD-1 with IC50 values of 0.18, 0.86, and 1.43 µM, respectively. MLN8054 also potently inhibits the growth of breast tumor cell lines MCF-7 and MDA-MB-231 with IC50 values of 0.67 and 0.74 µM, respectively. MLN8054 treatment (1 µM) results in G2/Maccumulation and spindle defects and inhibits proliferation in both HCT-116 colorectal and PC-3 prostate human tumor cells.^[1] Furthermore, MLN8054-treated HCT-116 cells frequently show alignment defects during metaphase, lagging chromosomes in anaphase, and chromatin bridges during telophase.^[2] In HCT-116 and PC-3 human xenografts models, MLN8054 (3, 10, and 30 mg/kg) has a dose-dependent tumor growth inhibition (TGI) compared with vehicle-treated mice. In PC-3 tumor xenograft model, MLN8054 doses of 30 mg/kg once a day has a TGI of 81% and MLN8054 doses of 30 mg/kg twice a day has a TGI of 93%.^[1] In additional models including the PC3 prostate and Calu-6 lung human tumor xenografts, MLN8054 (30 mg/kg) also has a significantly tumor growth inhibition.^[3]

Protocols

In vivo: MLN8054 is dissolved in distilled water.^[2]

References

[1] Manfredi MG, et al. Antitumor activity of MLN8054, an orally active small-molecule inhibitor of Aurora A kinase. Proc Natl Acad Sci U S A. 2007, 104(10): 4106-4111. [2] Hoar K, et al. MLN8054, a small-molecule inhibitor of Aurora A, causes spindle pole and chromosome congression defects leading to aneuploidy. Mol Cell Biol. 2007, 27(12): 4513-4525. [3] Jessica Huck, et al. Preclinical antitumor activity with MLN8054, a small molecule Aurora A kinase inhibitor. Proc Amer Assoc Cancer Res. 2006, 47.

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