MSC2530818

Igama Lekhemikhali:

[(2S)-2-(4-Chlorophenyl)pyrrolidin-1-yl]-(3-methyl-1H-pyrazolo[3,4-b]pyridin-5-yl)methanone

Ikhodi ye-SMILES:

O=C(N1[C@H](C2=CC=C(Cl)C=C2)CCC1)C3=CN=C(NN=C4C)C4=C3

Ikhodi ye-InChi:

I-InChI=1S/C18H17ClN4O/c1-11-15-9-13(10-20-17(15)22-21-11)18(24)23-8-2-3-16(23)12-4- 6-14(19)7-5-12/h4-7,9-10,16H,2-3,8H2,1H3,(H,20,21,22)/t16-/m0/s1

I-InChi Key:

ODRITQGYYWHQGM-INIZCTEOSA-N

Igama elingukhiye:

MSC2530818, MSC-2530818, MSC 2530818, 1883423-59-3

Ukunyibilika:I-Soluble ku-DMSO

Isitoreji:0 - 4°C isikhathi esifushane (izinsuku ukuya emavikini), noma -20°C isikhathi eside (izinyanga).

Incazelo:

I-MSC2530818 iyi-CDK8 Inhibitor Enamandla, Ekhethayo, kanye ne-Olly Bioavailable Bioavailable ene-CDK8 IC50 = 2.6 nM; Ukubikezela kwe-PK yomuntu: Cl ~ 0.14 L/H/Kg; t1/2 ~ 2.4h; F > 75%. I-MSC2530818 ibonisa ukukhetha okuhle kakhulu kwe-kinase, amandla e-biochemical kanye namaselula, ukuzinza kwe-microsomal, futhi itholakala ngomlomo nge-bioavailable. I-MSC2530818 ikhombisa amandla afanelekile nokukhetha ukuze kuthuthukele ku-preclinical in vivo efficacy kanye nezifundo zokuphepha.

Ithagethi: CDK