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MLN-8237

Description In vitro In vivo
MLN-8237
MLN-8237 structure
CAS No.
1028486-01-2
Chemical Name:
MLN-8237
Synonyms
MLN-823;MLN-8237;Alisertib;MLN8237 (Alisertib);Alisertib (MLN8237);Fluorocyclopentenylcytosine;MLN 8237 (Contain 10% DMSO);alisertib (auroura A kinase inhibitor);4-((9-Chloro-7-(2-fluoro-6-methoxyphenyl)-5H-benzo[c]pyrimido-[4,5-e]azepin-2-yl)amino)-2-meth;4-((9-Chloro-7-(2-fluoro-6-methoxyphenyl)-5H-benzo[c]pyrimido-[4,5-e]azepin-2-yl)amino)-2-methoxy
CBNumber:
CB62510095
Molecular Formula:
C27H20ClFN4O4
Formula Weight:
518.9235032
MOL File:
1028486-01-2.mol

MLN-8237 price More Price(3)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 13602 MLN8237 ≥98% 1028486-01-2 1mg $25 2018-11-13 Buy
Cayman Chemical 13602 MLN8237 ≥98% 1028486-01-2 5mg $106 2018-11-13 Buy
Cayman Chemical 13602 MLN8237 ≥98% 1028486-01-2 10mg $188 2018-11-13 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.

Chemical Properties

Off-White Solid

Uses

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

MLN-8237 Preparation Products And Raw materials

Raw materials

Preparation Products


MLN-8237 Suppliers

Global( 98)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
ATK CHEMICAL COMPANY LIMITED
+86 21 5161 9050/ 5187 7795
+86 21 5161 9052/ 5187 7796 ivan@atkchemical.com CHINA 24191 60
Capot Chemical Co.,Ltd.
+86 (0)571-855 867 18
+86 (0)571-858 647 95 sales@capotchem.com China 19918 60
career henan chemical co
+86-371-86658258
sales@coreychem.com CHINA 29979 58
Biochempartner
0086-13720134139
candy@biochempartner.com CHINA 969 58
Hubei xin bonus chemical co. LTD
86-13657291602
027-59338440 sales@guangaobio.com CHINA 23049 58
BOC Sciences
1-631-619-7922
1-631-614-7828 inquiry@bocsci.com United States 20115 58
Chongqing Chemdad Co., Ltd
+86-13650506873
sales@chemdad.com CHINA 30864 58
Shanghai SuperLan Chemcial Technique Centre +86-21-5160 1219, +86-15618227136
+86-21-5160 1218 sales@SuperLan-chem.com China 1897 58
Shanghai Boyle Chemical Co., Ltd.
86-21-57758967 sales@boylechem.com China 2926 55
J & K SCIENTIFIC LTD. 400-666-7788 +86-10-82848833
86-10-82849933 jkinfo@jkchemical.com;market6@jkchemical.com China 96815 76

View Lastest Price from MLN-8237 manufacturers

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

1028486-01-2(MLN-8237)Related Search:


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  • 1028486-01-2
  • C27H20ClFN4O4
  • Inhibitors
  • Intermediates & Fine Chemicals
  • Pharmaceuticals
  • Inhibitor
  • API
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