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
- Molecular Weight:
- 518.92
- MDL Number:
- MFCD16621243
- MOL File:
- 1028486-01-2.mol
| 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. |
| FDA UNII | T66ES73M18 |
| NCI Drug Dictionary | alisertib |
SAFETY
Risk and Safety Statements
| Signal word | Warning | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Hazard statements | H320 | |||||||||
| Precautionary statements | P264-P305+P351+P338-P337+P313 | |||||||||
| NFPA 704 |
|
MLN-8237 price More Price(32)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 13602 | MLN8237 ≥98% | 1028486-01-2 | 1mg | $32 | 2024-03-01 | Buy |
| Cayman Chemical | 13602 | MLN8237 ≥98% | 1028486-01-2 | 5mg | $131 | 2024-03-01 | Buy |
| Cayman Chemical | 13602 | MLN8237 ≥98% | 1028486-01-2 | 10mg | $230 | 2024-03-01 | Buy |
| Usbiological | 017705 | MLN 8237 | 1028486-01-2 | 5mg | $496 | 2021-12-16 | Buy |
| Medical Isotopes, Inc. | 66294 | MLN8237(Contain10%DMSO) | 1028486-01-2 | 5mg | $675 | 2021-12-16 | Buy |
MLN-8237 Chemical Properties,Uses,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
1of2
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Capot Chemical Co.,Ltd. | 571-85586718 +8613336195806 | sales@capotchem.com | China | 29797 | 60 |
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32480 | 60 |
| career henan chemical co | +86-0371-86658258 | sales@coreychem.com | China | 29914 | 58 |
| Biochempartner | 0086-13720134139 | candy@biochempartner.com | CHINA | 967 | 58 |
| Hubei xin bonus chemical co. LTD | 86-13657291602 | linda@hubeijusheng.com | CHINA | 22968 | 58 |
| BOC Sciences | +1-631-485-4226 | inquiry@bocsci.com | United States | 19553 | 58 |
| Chongqing Chemdad Co., Ltd | +86-023-61398051 +8613650506873 | sales@chemdad.com | China | 39916 | 58 |
| Alchem Pharmtech,Inc. | 8485655694 | sales@alchempharmtech.com | United States | 63711 | 58 |
| CONIER CHEM AND PHARMA LIMITED | +8618523575427 | sales@conier.com | China | 47465 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
View Lastest Price from MLN-8237 manufacturers
| Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
|---|---|---|---|---|---|---|---|---|
![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) pictures](/ProductImageEN/2023-04/Small/8ccce3f2-24d6-4f6d-b875-b0ab43be875a.jpg) |
2023-04-21 | 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
|
US $50.00 / kg | 1kg | 99% | 100 tons | Hebei Duling International Trade Co. LTD | |
 |
2021-10-08 | MLN8237 ;Alisertib
1028486-01-2
|
US $0.00-0.00 / g | 1g | 98% | 100kgs | Wuhan Nutra Biotechnology Co.,Ltd | |
 |
2019-07-06 | MLN-8237
1028486-01-2
|
US $1.00 / KG | 1G | 98% | 100KG | Career Henan Chemical Co |
-
- 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
- US $50.00 / kg
- 99%
- Hebei Duling International Trade Co. LTD
-
- MLN8237 ;Alisertib
1028486-01-2
- US $0.00-0.00 / g
- 98%
- Wuhan Nutra Biotechnology Co.,Ltd
-
- MLN-8237
1028486-01-2
- US $1.00 / KG
- 98%
- Career Henan Chemical Co