EED226

Igama leMchiza:

N-(furan-2-ylmethyl)-8-(4-(methylsulfonyl)phenyl)-[1,2,4]triazolo[4,3-c]pyrimidin-5-amine

Ikhowudi yoncumo:

O=S(C1=CC=C(C2=CN=C(NCC3=CC=CO3)N4C2=NN=C4)C=C1)(C)=O

Ikhowudi ye-InChi:

InChI=1S/C17H15N5O3S/c1-26(23,24)14-6-4-12(5-7-14)15-10-19-17(22-1 1-20-21-16(15)22)18-9-13-3-2-8-25-13/h2-8,10-11H,9H2,1H3,(H,18,19)

Isitshixo se-InChi:

DYIRSNMPIZZNBK-UHFFFAOYSA-N

Igama elingundoqo:

EED226, EED-226, EED 226, 2083627-02-3

Ukunyibilika:Inyibilika kwi-DMSO

Ugcino:0 - 4°C ixesha elifutshane (iintsuku ukuya kwiiveki), okanye -20°C ixesha elide (iinyanga).

Inkcazo:

I-EED226 yi-inhibitor enamandla kakhulu, esebenzayo kwaye ekhethiweyo ye-EZH2 kunye ne-EZH1 evavanyiwe ngokuchasene noluhlu olubanzi lweethagethi ze-epigenetic kunye ne-non-epigenetic. Inciphisa ngokubonakalayo uphawu lwehlabathi lwe-H3K27Me3 kwiiseli kwaye ibonise iziphumo ezikhethiweyo zokubulala iiseli kwiiseli eziphethe i-heterozygous Y641N mutation. I-EED226 inokungena okuphakathi njengoko kulinganiswe kwiiseli zeCaco-2 kwi-A→B=3.0x10-6 cm/s, kunye ne-efflux ratio kwi-7.6[1].

Ithagethi: EED226