MLN8237 (Alisertib)

Catalog No. A10004

MLN8237 (Alisertib) is a selective Aurora A inhibitor with IC50 of 1.2 nM in a cell-free assay. It has >200-fold higher selectivity for Aurora A than Aurora B. Phase 3..

Product Citations

Kimura M, .et al. Aurora A regulates the architecture of the Golgi apparatus, Exp Cell Res, 2018, Jun 1;367(1):73-80 PMID: 29571950
Jing Wang, .et al. The Aurora-A-Twist1 axis promotes highly aggressive phenotypes in pancreatic carcinoma, J Cell Sci, 2017, Mar 15; 130(6): 1078-1093 PMID: 28167680
Lessing D, .et al. A high-throughput small molecule screen identifies synergism between DNA methylation and Aurora kinase pathways for X reactivation, Proc Natl Acad Sci U S A, 2016, Dec 13;113(50):14366-14371 PMID: 28182563
Jennifer M. Sahni, .et al. Bromodomain and Extraterminal Protein Inhibition Blocks Growth of Triple-negative Breast Cancers through the Suppression of Aurora Kinases, J Biol Chem, 2016, Nov 4; 291(45): 23756-23768 PMID: 27650498

Technical details

Catalog Num	A10004
M. Wt	518.9
Formula	C27H20ClFN4O4
Purity	>98%
Storage	at -20°C 3 years Powder
CAS No.	1028486-01-2
Synonyms	N/A
SMILES	COC1=C(C(=CC=C1)F)C2=NCC3=CN=C(N=C3C4=C2C=C(C=C4)Cl)NC5=CC(=C(C=C5)C(=O)O)OC

Biological Activity

MLN8237 (Alisertib) is a selective Aurora A inhibitor with IC50 of 1.2 nM in a cell-free assay. It has >200-fold higher selectivity for Aurora A than Aurora B. Phase 3..

Solubility *

In vitro (25°C)	DMSO	27 mg/mL (52.03 mM)
	Water	<1 mg/mL (<1 mM)
	Ethanol	<1 mg/mL (<1 mM)
In vivo	15% Captisol	30 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Preparing Stock Solutions

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.1 mM	19.27 mL	96.36 mL	192.72 mL
0.5 mM	3.85 mL	19.27 mL	38.54 mL
1 mM	1.93 mL	9.64 mL	19.27 mL
5 mM	0.39 mL	1.93 mL	3.85 mL

*The above data is based on the productmolecular weight 518.9. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.