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Home > Inhibitors & Agonists > Ras-Raf-MAPK-ERK > MEK (MAP2K)

BI-847325

  Cat. No.:  DC8401   Featured
Chemical Structure
1207293-36-4
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More than 5000 active chemicals with high quality for research!
Field of application
BI-847325 is an orally bioavailable, and selective dual MEK/Aurora kinase inhibitor with IC50 of 3 nM, 25 nM, 15 nM, 25 nM, and 4 nM for Xenopus laevis Aurora B, human Aurora A and Aurora C, as well as human MEK1 and MEK2, respectively. Phase 1.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1207293-36-4
Chemical Name: 3-[3-[N-[4-[(Dimethylamino)methyl]phenyl]-C-phenylcarbonimidoyl]-2-hydroxy-1H-indol-6-yl]-N-ethylprop-2-ynamide
Synonyms: BI-847325;BI847325;3-[3-[[[4-[(Dimethylamino)methyl]phenyl]amino]phenylmethylene]-2,3-dihydro-2-oxo-1H-indol-6-yl]-N-ethyl-2-propynamide;hylpropiolamide;BI 847325;(Z)-3-(3-(((4-((dimethylamino)methyl)phenyl)amino)(phenyl)methylene)-2-oxoindolin-6-yl)-N-ethylpropiolamide;3-[(3~{z})-3-[[[4-[(Dimethylamino)methyl]phenyl]amino]-Phenyl-Methylidene]-2-Oxidanylidene-1~{h}-Indol-6-Yl]-~{n}-Ethyl-Prop-2-Ynamide;5U5;BDBM142744;BCP15994;s7843;AK198901;US893709;3-[3-[N-[4-[(Dimethylamino)methyl]phenyl]-C-phenylcarbonimidoyl]-2-hydroxy-1H-indol-6-yl]-N-ethylpro
SMILES: O([H])C1=C(/C(/C2C([H])=C([H])C([H])=C([H])C=2[H])=N/C2C([H])=C([H])C(=C([H])C=2[H])C([H])([H])N(C([H])([H])[H])C([H])([H])[H])C2C([H])=C([H])C(C#CC(N([H])C([H])([H])C([H])([H])[H])=O)=C([H])C=2N1[H]
Formula: C29H28N4O2
M.Wt: 464.5582
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: BI-847325 is an ATP competitive dual inhibitor of MEK and aurora kinases (AK) with IC50 values of 4 and 15 nM for human MEK2 and AK-C, respectively.
In Vivo: Daily oral administration of BI 847325 at 10 mg/kg shows efficacy in both BRAF- and KRAS-mutant xenograft models. BI 847325 administered once weekly at 70 mg/kg inhibits both MEK and AK in KRAS-mutant tumors[1].
In Vitro: BI 847325 inhibits the activity of X. laevis AK-B with an IC50 of 3 nM; the IC50 values for human AK-A and AK-C are 25 and 15 nM, respectively. BI 847325 also inhibits human MEK1 and MEK2 with respective IC50 values of 25 and 4 nM. BI 847325 at 1,000 nM inhibits 6 enzymes by more than 50% (LCK, MAP3K8, FGFR1, AMPK, CAMK1D and TBK1) and the IC50 values are below 100 nM only for LCK (5 nM) and MAP3K8 (93 nM). Proliferation is inhibited in A375 and Calu-6 cell lines with GI50 values of 7.5 nM and 60 nM, respectively[1].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
DC7488 RO4987655 RO4987655(CH-4987655) is an orally active small molecule, targeting mitogen-activated protein kinase kinase 1 (MAP2K1/MEK1 IC50=5.2 nM), with potential antineoplastic activity.
DC7308 TAK-733 TAK-733 is a potent and selective MEK allosteric site inhibitor for MEK1 with IC50 of 3.2 nM, inactive to Abl1, AKT3, c-RAF, CamK1, CDK2, c-Met, etc.
DC8401 BI-847325 BI-847325 is an orally bioavailable, and selective dual MEK/Aurora kinase inhibitor with IC50 of 3 nM, 25 nM, 15 nM, 25 nM, and 4 nM for Xenopus laevis Aurora B, human Aurora A and Aurora C, as well as human MEK1 and MEK2, respectively. Phase 1.
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