Name: BI-847325
CAS#: 1207293-36-4
Chemical Formula: C29H28N4O2
Exact Mass: 464.2212
Molecular Weight: 464.569
Elemental Analysis: C, 74.98; H, 6.08; N, 12.06; O, 6.89
EOS Med Chem produce BI-847325,1207293-36-4 in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.
BI-847325,1207293-36-4 Intermediates, EOS Med Chem have 8; BI-847325,1207293-36-4 Impurity we have 10, all from GMP, FDA plant.
Now BI-847325,1207293-36-4 DMF document is preparing.
Until 2016, Aug, BI-847325,1207293-36-4 more than produced 25kg API, 120kg Intermediates
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BI-847325 BI-847325 1207293-36-4
BI-847325 Intermediates N-ethylpropiolamide 2682-33-9
BI-847325 Intermediates 6-iodoindolin-2-one 919103-45-0
BI-847325 Intermediates (E)-3-(hydroxy(phenyl)methylene)-6-iodoindolin-2-one 1535204-23-9
BI-847325 Intermediates (E)-6-iodo-3-(phenyl((trimethylsilyl)oxy)methylene)-2-((trimethylsilyl)oxy)-3H-indole
BI-847325 Intermediates (Z)-3-(((4-((dimethylamino)methyl)phenyl)amino)(phenyl)methylene)-6-iodoindolin-2-one 1537909-08-2
Description: BI-847325 is an orally available dual inhibitor of mitogen-activated protein kinase kinase (MEK) and Aurora kinases, with potential antineoplastic activity. Upon oral administration, MEK/Aurora kinase inhibitor BI 847325 selectively binds to and inhibits the activity of MEK, which both prevents the activation of MEK-dependent effector proteins and inhibits growth factor-mediated cell signaling. BI 847325 also binds to and inhibits the activity of the Aurora kinases A, B and C which may disrupt the assembly of the mitotic spindle apparatus, prevent chromosome segregation, and inhibit both cellular division and proliferation in Aurora kinase-overexpressing tumor cells.
Synonym: BI-847325; BI 847325; BI847325.
IUPAC/Chemical Name: (Z)-3-(3-((4-((dimethylamino)methyl)phenylamino)(phenyl)methylene)-2-oxoindolin-6-yl)-N-ethylpropiolamide
SMILES Code: O=C(NCC)C#CC1=CC(NC/2=O)=C(C=C1)C2=C(NC3=CC=C(CN(C)C)C=C3)/C4=CC=CC=C4
1: Schöffski P, Aftimos P, Dumez H, Deleporte A, De Block K, Costermans J,
Billiet M, Meeus MA, Lee C, Schnell D, Goeldner RG, Awada A. A phase I study of
two dosing schedules of oral BI 847325 in patients with advanced solid tumors.
Cancer Chemother Pharmacol. 2016 Jan;77(1):99-108. doi:
10.1007/s00280-015-2914-5. Epub 2015 Dec 9. PubMed PMID: 26650227.
2: Phadke MS, Sini P, Smalley KS. The Novel ATP-Competitive MEK/Aurora Kinase
Inhibitor BI-847325 Overcomes Acquired BRAF Inhibitor Resistance through
Suppression of Mcl-1 and MEK Expression. Mol Cancer Ther. 2015 Jun;14(6):1354-64.
doi: 10.1158/1535-7163.MCT-14-0832. Epub 2015 Apr 14. PubMed PMID: 25873592;
PubMed Central PMCID: PMC4458462.
