Grouped product items

SKU

Size

Availability

Price

Qty

A126379-5mg

5mg

Available within 4-8 weeks(?)

$70.90

A126379-25mg

25mg

Available within 4-8 weeks(?)

$319.90

A126379-100mg

100mg

Available within 4-8 weeks(?)

$444.90

Basic Description

Synonyms	Alisertib\|1028486-01-2\|MLN8237\|MLN-8237\|MLN 8237\|MLN8237 (Alisertib)\|4-((9-Chloro-7-(2-fluoro-6-methoxyphenyl)-5H-benzo[c]pyrimido[4,5-e]azepin-2-yl)amino)-2-methoxybenzoic acid\|Alisertib [USAN]\|4-[[9-Chloro-7-(2-fluoro-6-methoxyphenyl)-5H-pyrimido[5,4-d]
Specifications & Purity	Moligand™, ≥98%
Biochemical and Physiological Mechanisms	Alisertib is a selective Aurora kinase A inhibitor with a median IC50 of 61 nM. Alisertib is a second-generation, orally bioavailable, highly selective small molecule inhibitor of the Aurora A kinase (serine/threonine protein kinase) with potential antine
Storage Temp	Store at -20°C
Shipped In	Ice chest + Ice pads
Grade	Moligand™
Action Type	INHIBITOR
Mechanism of action	Serine/threonine-protein kinase Aurora-A inhibitor
Note	25mg卖完停产，不再备货
Product Description	Alisertib (MLN8237) is a selective Aurora A inhibitor with IC50 of 1.2 nM; has >200-fold higher selectivity for Aurora A than Aurora B.

Product Properties

ALogP	5

Associated Targets

CTH Tchem Cystathionine gamma-lyase 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CDK1 Tchem Cyclin-dependent kinase 1 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ERBB4 Tclin Receptor tyrosine-protein kinase erbB-4 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

EPHB6 Tchem Ephrin type-B receptor 6 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ERBB2 Tclin Receptor tyrosine-protein kinase erbB-2 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

GABRA1 Tclin Gamma-aminobutyric acid receptor subunit alpha-1 1 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

EGFR Tclin Epidermal growth factor receptor 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

DNAJA1 Tchem DnaJ homolog subfamily A member 1 1 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CDK9 Tchem Cyclin-dependent kinase 9 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CDK16 Tchem Cyclin-dependent kinase 16 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CDK17 Tchem Cyclin-dependent kinase 17 0 Activities

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CDK2 Tchem Cyclin-dependent kinase 2 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CDK5 Tchem Cyclin-dependent-like kinase 5 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

YES1 Tclin Tyrosine-protein kinase Yes 0 Activities

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TYK2 Tclin Non-receptor tyrosine-protein kinase TYK2 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HDAC6 Tclin Histone deacetylase 6 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

FLT3 Tclin Receptor-type tyrosine-protein kinase FLT3 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

FGFR1 Tclin Fibroblast growth factor receptor 1 0 Activities

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FGFR3 Tclin Fibroblast growth factor receptor 3 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

MET Tclin Hepatocyte growth factor receptor 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

IGF1R Tclin Insulin-like growth factor 1 receptor 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

JAK3 Tclin Tyrosine-protein kinase JAK3 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PRKACG Tchem cAMP-dependent protein kinase catalytic subunit gamma 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PLK4 Tchem Serine/threonine-protein kinase PLK4 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PIM1 Tchem Serine/threonine-protein kinase pim-1 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PDGFRA Tclin Platelet-derived growth factor receptor alpha 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PIM2 Tchem Serine/threonine-protein kinase pim-2 0 Activities

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PIM3 Tchem Serine/threonine-protein kinase pim-3 0 Activities

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PRKG2 Tchem cGMP-dependent protein kinase 2 0 Activities

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BMPR1B Tchem Bone morphogenetic protein receptor type-1B 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

BTK Tclin Tyrosine-protein kinase BTK 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

AURKA Tchem Aurora kinase A 15 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

AURKB Tchem Aurora kinase B 2 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

FLT1 Tclin Vascular endothelial growth factor receptor 1 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

KDR Tclin Vascular endothelial growth factor receptor 2 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

AAK1 Tchem AP2-associated protein kinase 1 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

TNK2 Tclin Activated CDC42 kinase 1 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ABL1 Tclin Tyrosine-protein kinase ABL1 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

AKT3 Tchem RAC-gamma serine/threonine-protein kinase 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

AKT2 Tchem RAC-beta serine/threonine-protein kinase 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

AKT1 Tchem RAC-alpha serine/threonine-protein kinase 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CLK3 Tchem Dual specificity protein kinase CLK3 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CLK1 Tchem Dual specificity protein kinase CLK1 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

GSK3B Tclin Glycogen synthase kinase-3 beta 0 Activities

Discover Target: GSK3B

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

GSK3A Tclin Glycogen synthase kinase-3 alpha 0 Activities

Discover Target: GSK3A

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

KIT Tclin Mast/stem cell growth factor receptor Kit 0 Activities

Discover Target: KIT

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

NTRK1 Tclin High affinity nerve growth factor receptor 0 Activities

Discover Target: NTRK1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

MAP2K1 Tclin Dual specificity mitogen-activated protein kinase kinase 1 0 Activities

Discover Target: MAP2K1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Names and Identifiers

IUPAC Name	4-[[9-chloro-7-(2-fluoro-6-methoxyphenyl)-5H-pyrimido[5,4-d][2]benzazepin-2-yl]amino]-2-methoxybenzoic acid
INCHI	InChI=1S/C27H20ClFN4O4/c1-36-21-5-3-4-20(29)23(21)25-19-10-15(28)6-8-17(19)24-14(12-30-25)13-31-27(33-24)32-16-7-9-18(26(34)35)22(11-16)37-2/h3-11,13H,12H2,1-2H3,(H,34,35)(H,31,32,33)
InChi Key	ZLHFILGSQDJULK-UHFFFAOYSA-N
Canonical 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
Isomeric 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
PubChem CID	24771867
Molecular Weight	518.94

Database links

PubChem CID	24771867
ChEMBL Ligand	CHEMBL483158
Wikipedia	Alisertib
CAS Registry No.	1028486-01-2
RCSB PDB Ligand	A5B

Certificates

Certificate of Analysis(COA)

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To view the certificate results,please click on a Lot number.For Lot numbers from past orders,please use our order status section

1 results found

Lot Number	Certificate Type	Date	Item
D1725126	Certificate of Analysis	Nov 16, 2022	A126379

Chemical and Physical Properties

Solubility	DMSO ≥42mg/mL Water <1.2mg/mL Ethanol <1.2mg/mL

References

1. Görgün G, Calabrese E, Hideshima T, Ecsedy J, Perrone G, Mani M, Ikeda H, Bianchi G, Hu Y, Cirstea D et al.. (2010) A novel Aurora-A kinase inhibitor MLN8237 induces cytotoxicity and cell-cycle arrest in multiple myeloma.. Blood, 115 (25): (5202-13). [PMID:20382844]
2. Sloane DA, Trikic MZ, Chu ML, Lamers MB, Mason CS, Mueller I, Savory WJ, Williams DH, Eyers PA. (2010) Drug-resistant aurora A mutants for cellular target validation of the small molecule kinase inhibitors MLN8054 and MLN8237.. ACS Chem Biol, 5 (6): (563-76). [PMID:20426425]

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SKU	Size	Availability	Price
A126379-5mg	5mg	Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!	$70.90
A126379-25mg	25mg	Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!	$319.90
A126379-100mg	100mg	Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!	$444.90

Alisertib (MLN8237) - ≥98%, high purity , Serine/threonine-protein kinase Aurora-A inhibitor, CAS No.1028486-01-2, Serine/threonine-protein kinase Aurora-A inhibitor

Basic Description

Product Properties

Associated Targets

CTH Tchem Cystathionine gamma-lyase 0 Activities

CDK1 Tchem Cyclin-dependent kinase 1 0 Activities

ERBB4 Tclin Receptor tyrosine-protein kinase erbB-4 0 Activities

EPHB6 Tchem Ephrin type-B receptor 6 0 Activities

ERBB2 Tclin Receptor tyrosine-protein kinase erbB-2 0 Activities

GABRA1 Tclin Gamma-aminobutyric acid receptor subunit alpha-1 1 Activities

EGFR Tclin Epidermal growth factor receptor 0 Activities

DNAJA1 Tchem DnaJ homolog subfamily A member 1 1 Activities

CDK9 Tchem Cyclin-dependent kinase 9 0 Activities

CDK16 Tchem Cyclin-dependent kinase 16 0 Activities

CDK17 Tchem Cyclin-dependent kinase 17 0 Activities

CDK2 Tchem Cyclin-dependent kinase 2 0 Activities

CDK5 Tchem Cyclin-dependent-like kinase 5 0 Activities

YES1 Tclin Tyrosine-protein kinase Yes 0 Activities

TYK2 Tclin Non-receptor tyrosine-protein kinase TYK2 0 Activities

HDAC6 Tclin Histone deacetylase 6 0 Activities

FLT3 Tclin Receptor-type tyrosine-protein kinase FLT3 0 Activities

FGFR1 Tclin Fibroblast growth factor receptor 1 0 Activities

FGFR3 Tclin Fibroblast growth factor receptor 3 0 Activities

MET Tclin Hepatocyte growth factor receptor 0 Activities

IGF1R Tclin Insulin-like growth factor 1 receptor 0 Activities

JAK3 Tclin Tyrosine-protein kinase JAK3 0 Activities

PRKACG Tchem cAMP-dependent protein kinase catalytic subunit gamma 0 Activities

PLK4 Tchem Serine/threonine-protein kinase PLK4 0 Activities

PIM1 Tchem Serine/threonine-protein kinase pim-1 0 Activities

PDGFRA Tclin Platelet-derived growth factor receptor alpha 0 Activities

PIM2 Tchem Serine/threonine-protein kinase pim-2 0 Activities

PIM3 Tchem Serine/threonine-protein kinase pim-3 0 Activities

PRKG2 Tchem cGMP-dependent protein kinase 2 0 Activities

BMPR1B Tchem Bone morphogenetic protein receptor type-1B 0 Activities

BTK Tclin Tyrosine-protein kinase BTK 0 Activities

AURKA Tchem Aurora kinase A 15 Activities

AURKB Tchem Aurora kinase B 2 Activities

FLT1 Tclin Vascular endothelial growth factor receptor 1 0 Activities

KDR Tclin Vascular endothelial growth factor receptor 2 0 Activities

AAK1 Tchem AP2-associated protein kinase 1 0 Activities

TNK2 Tclin Activated CDC42 kinase 1 0 Activities

ABL1 Tclin Tyrosine-protein kinase ABL1 0 Activities

AKT3 Tchem RAC-gamma serine/threonine-protein kinase 0 Activities

AKT2 Tchem RAC-beta serine/threonine-protein kinase 0 Activities

AKT1 Tchem RAC-alpha serine/threonine-protein kinase 0 Activities

CLK3 Tchem Dual specificity protein kinase CLK3 0 Activities

CLK1 Tchem Dual specificity protein kinase CLK1 0 Activities

GSK3B Tclin Glycogen synthase kinase-3 beta 0 Activities

GSK3A Tclin Glycogen synthase kinase-3 alpha 0 Activities

KIT Tclin Mast/stem cell growth factor receptor Kit 0 Activities

NTRK1 Tclin High affinity nerve growth factor receptor 0 Activities

MAP2K1 Tclin Dual specificity mitogen-activated protein kinase kinase 1 0 Activities

Names and Identifiers

Database links

Certificates

Certificate of Analysis(COA)

Chemical and Physical Properties

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References

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