3-[3-[[[4-[(Dimethylamino)methyl]phenyl]amino]phenylmethylene]-2,3-dihydro-2-oxo-1H-indol-6-yl]-N-ethyl-2-propynamide

Name	BI-847325
Synonyms	BI847325 BI-847325 BI 847325 3-[3-[[4-(dimethylaminomethyl)anilino]-phenylmethylidene]-2-oxo-1H-indol-6-yl]-N-ethylprop-2-ynamide (Z)-3-(3-(((4-((Dimethylamino)methyl)phenyl)amino)(phenyl)methylene)-2-oxoindolin-6-yl)-N-ethylpropiolamide 3-[3-[[[4-[(Dimethylamino)methyl]phenyl]amino]phenylmethylene]-2,3-dihydro-2-oxo-1H-indol-6-yl]-N-ethyl-2-propynamide 2-Propynamide, 3-[3-[[[4-[(dimethylamino)methyl]phenyl]amino]phenylmethylene]-2,3-dihydro-2-oxo-1H-indol-6-yl]-N-ethyl-
CAS	1207293-36-4

Molecular Formula	C29H28N4O2
Molar Mass	464.56
Solubility	DMSO: ≥36 mg/mL
Storage Condition	-20℃
In vitro study	BI-847325 showed growth inhibition in BRAF mutant and vemurafenib resistant melanoma cells with an IC50 in the range of 0.3 nM-2 μm and prevented colony formation in six BRAF mutant melanoma cell lines. BI-847325 also induces apoptosis by reducing Mcl-1 expression.
In vivo study	In mice loaded with 1205Lu and 1205LuR xenografts, BI-847325 (75 mg/kg, p.o.) caused significant tumor regression without significant change in body weight.

Last Update：2024-01-02 23:10:35

biological activity	BI-847325 is an oral selective dual MEK/Aurora kinase inhibitor with biological activity. the IC50 for Xenopus Aurora B, human Aurora A and Aurora C, and human MEK1 and MEK2 are 3 nM,25 nM,15 nM respectively, 25 nM, and 4 nM. Phase 1.
target	TargetValue Aurora B (Xenopus laevis) 3 nM MEK2 4 nM Aurora C (Human) 15 nM Aurora A (Human) 25 nM MEK1 25 nM
Target	Value
Aurora B (Xenopus laevis)	3 nM
MEK2	4 nM
Aurora C (Human)	15 nM
Aurora A (Human)	25 nM
MEK1	25 nM
in vitro study	BI-847325 showed growth inhibition on BRAF mutant and vemurafenib resistant melanoma cells, with IC50 ranging from 0.3 nM-2 μM and preventing colony formation in 6 BRAF mutant melanoma cell lines. BI-847325 also induce apoptosis by reducing Mcl-1 expression.
in vivo study	in mice loaded with 1205Lu and 1205LuR xenografts, BI-847325 (75 mg/kg, p.o.) caused significant tumor degeneration without significant weight change.

Last Update：2024-04-09 21:54:55

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CAS: 1207293-36-4
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Product Name: BI-847325 Visit Supplier Webpage Request for quotation
CAS: 1207293-36-4
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409

Wechat: 18301782025

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3-[3-[[[4-[(Dimethylamino)methyl]phenyl]amino]phenylmethylene]-2,3-dihydro-2-oxo-1H-indol-6-yl]-N-ethyl-2-propynamide Request for Quotation