MLN-8237

Description In vitro In vivo

Product Name: MLN-8237
CAS No.: 1028486-01-2
Chemical Name: MLN-8237
Synonyms: Alisertib;Alisertib (MLN8237);MLN8237 (Alisertib);CS-277;MLN-823;MLN-8237;MLN-8237; MLN 8237;MLN-8237 USP/EP/BP;13C,2H3]-Alisertib;ALIERTIB (MLN 8237)
CBNumber: CB62510095
Molecular Formula: C27H20ClFN4O4
Formula Weight: 518.92
MOL File: 1028486-01-2.mol

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MLN-8237 Property

Boiling point:: 729.1±70.0 °C(Predicted)
Density: 1.43±0.1 g/cm3(Predicted)
storage temp.: -20°C
solubility: Soluble in DMSO (up to 5 mg/ml)
form: solid
pka: 4.07±0.10(Predicted)
color: Off-white
Stability:: Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.

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Hazard and Precautionary Statements (GHS)

Signal word: Warning

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 13602
Product name: MLN8237
Purity: ≥98%
Packaging: 1mg
Price: $32
Updated: 2024/03/01

Cayman Chemical

Product number: 13602
Product name: MLN8237
Purity: ≥98%
Packaging: 5mg
Price: $131
Updated: 2024/03/01

Cayman Chemical

Product number: 13602
Product name: MLN8237
Purity: ≥98%
Packaging: 10mg
Price: $230
Updated: 2024/03/01

Usbiological

Product number: 017705
Product name: MLN 8237
Packaging: 5mg
Price: $496
Updated: 2021/12/16

Medical Isotopes, Inc.

Product number: 66294
Product name: MLN8237(Contain10%DMSO)
Packaging: 5mg
Price: $675
Updated: 2021/12/16

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MLN-8237 Chemical Properties,Usage,Production

Description

Alisertib (MLN8237) 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.

In vitro

MLN8237 shows >200-fold higher selectivity for Aurora A than the structurally related Aurora B with an IC50 of 396.5 nM, and does not have any significant activity against 205 other kinases. [1] MLN8237 (0.5 μM) treatment inhibits the phosphorylation of Aurora A in MM1.S and OPM1 cells, without affecting the Aurora B mediated histone H3 phosphorylation. MLN8237 significantly inhibits cell proliferation in multiple myeloma (MM) cell lines with IC50 values of 0.003-1.71 μM. MLN8237 displays more potent anti-proliferation activity against primary MM cells and MM cell lines in the presence of BM stroma cells, as well as IL-6 and IGF-1 than against MM cells alone. MLN8237 (0.5 μM) induces 2- to 6-fold increase in G2/M phase in primary MM cells and cell lines, as well as significant apoptosis and senescence, involving the up-regulation of p53, p21 and p27, as well as PARP, caspase 3, and caspase 9 cleavage. In addition, MLN8237 shows strong synergistic anti-MM effect with dexamethasone, as well as additive effect with doxorubicin and bortezomib.MLN8237 (0.5 μM) treatment causes the inhibition of colony formation of FLO-1, OE19, and OE33 esophageal adenocarinoma cell lines, and induces a significant increase in the percentage of polyploid cells, and subsequently an increase in the percentage of cells in the sub-G1 phase, which can be further enhanced in combination with cisplatin (2.5 μM), involving the higher induction of TAp73β, PUMA, NOXA, cleaved caspase-3, and cleaved PARP as compared with a single-agent treatment.

In vivo

MLN8237 significantly reduces the tumor burden with tumor growth inhibition (TGI) of 42% and 80% at 15 mg/kg and 30 mg/kg, respectively, and prolongs the survival of mice compared with the control.

Description

Alisertib (MLN8237, 1028486-01-2) is a highly selective and potent (IC50?= 1 nM) cell permeable inhibitor of Aurora A with off-target binding at GABAA?(IC50?= 490 nM).1?It disrupts the Aurora A-Myc complex leading to Myc degradation2?in Myc amplified neuroblastomas3?and p53-mutant human hepatocellular carcinoma cell4. Alisertib has been found to induce apoptosis and autophagy in breast cancer5?and melanoma6?cells?via?suppression of activation of the p38 MAPK pathway.

Chemical Properties

Off-White Solid

Uses

An Aurora kinase inhibitor, used to treat patients with advanced solid tumors.

Definition

ChEBI: 4-[[9-chloro-7-(2-fluoro-6-methoxyphenyl)-5H-pyrimido[5,4-d][2]benzazepin-2-yl]amino]-2-methoxybenzoic acid is a benzazepine.

target

Aurora A

References

1) Sells?et al.?(2015),?MLN8054 and Alisertib (MLN8237):Discovery of Selective Oral Aurora A Inhibitors; ACS Med. Chem. Lett.?6?630 2) Richards?et al.?(2016),?Structural basis of N-Myc binding by Aurora-A and its destabilization by kinase inhibitors; Proc. Natl. Acad. Sci. USA?113?13726 3) Brockmann?et al.?(2013),?Small molecule inhibitors of aurora-a induce proteasomal degradation of N-myc in childhood neuroblastoma; Cancer Cell?24?75 4) Dauch?et al.?(2016),?A MYC-aurora kinase A protein complex represents an actionable drug target in p53-altered liver cancer; Nat. Med.?22?744 5) Li?et al.?(2015),?The investigational Aurora kinase A inhibitor alisertib (MLN8237) induces cell cycle G2/M arrest, apoptosis, and autophagy via p38 MAPK and Akt/mTOR signaling pathways in human breast cancer cells; Drug Des. Devel. Ther.?16?1627 6) Shang?et al.?(2017),?Alisertib promotes apoptosis and autophagy in melanoma through p38 MAPK-mediated aurora a signaling; Oncotarget?8?107076

MLN-8237 Preparation Products And Raw materials

Raw materials

Preparation Products

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MLN-8237 Suppliers

Canada 1 China 158 India 3 United States 22 Global 184

AdooQ BioScience, LLC

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Cckinase, Inc.

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View Lastest Price from MLN-8237 manufacturers

Wuhan Nutra Biotechnology Co.,Ltd

Product: MLN8237 ;Alisertib 1028486-01-2
Price: US $0.00-0.00/g
Min. Order: 1g
Purity: 98%
Supply Ability: 100kgs
Release date: 2021-05-23

Career Henan Chemical Co

Product: MLN-8237 1028486-01-2
Price: US $1.00/KG
Min. Order: 1G
Purity: 98%
Supply Ability: 100KG
Release date: 2018-08-21

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Benzoic acid, 4-[[9-chloro-7-(2-fluoro-6-methoxyphenyl)-5H-pyrimido[5,4-d][2]benzazepin-2-yl]amino]-2-methoxy-

MLN-8237 4-[[9-Chloro-7-(2-fluoro-6-methoxyphenyl)-5H-pyrimido[5,4-d][2]benzazepin-2-yl]amino]-2-methoxybenzoic acid

alisertib (auroura A kinase inhibitor)

Fluorocyclopentenylcytosine

ALISERTIB (MLN8237);MLN 8237; MLN8237;MLN-8237

4-((9-Chloro-7-(2-fluoro-6-methoxyphenyl)-5H-benzo[c]pyrimido-[4,5-e]azepin-2-yl)amino)-2-meth

MLN-823

MLN-8237

4-((9-chloro-7-(2-fluoro-6-Methoxyphenyl)-5H-benzo[c]pyriMido[4,5-e]azepin-2-yl)aMino)-2-Methoxybenzoic acid

MLN8237 (Alisertib)

Alisertib

4-[[9-Chloro-7-(2-fluoro-6-methoxyphenyl)-5H-pyrimido[5,4-d][2]benzazepin-2-yl]amino]-2-methoxybenzoic acid

Alisertib (MLN8237)

4-((9-Chloro-7-(2-fluoro-6-methoxyphenyl)-5H-benzo[c]pyrimido-[4,5-e]azepin-2-yl)amino)-2-methoxy

MLN 8237 (Contain 10% DMSO)

MLN-8237; MLN 8237

CS-277

ALIERTIB (MLN 8237)

ALISERTIB;MLN 8237;MLN-8237

MLN-8237 USP/EP/BP

13C,2H3]-Alisertib

MLN8237 Alisertib MLN-8237

arrest,myeloma,cytotoxicity,MLN-8237,spindle,Alisertib,inhibit,mitotic,Autophagy,Aurora Kinase,cancer,multiple,Inhibitor,MLN8237,cell-cycle,Apoptosis

4-((9-Chloro-7-(2-fluoro-6-methoxyphenyl)-5H-benzo[c]pyrimido-[4,5-e]azepin-2-yl)amino)-2-methoxy MLN 8237 (Contain 10% DMSO)

1028486-01-2

C27H20ClFN4O4

Inhibitor

Inhibitors

Intermediates & Fine Chemicals

Pharmaceuticals

API