I-Quizartinib; I-AC-010220; I-AC-220

Igama Lekhemikhali:

N-(5-tert-Butylisoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-ylethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl ]phenyl}urea

Ikhodi ye-SMILES:

O=C(NC1=CC=C(C2=CN3C(SC4=CC(OCCN5CCOCC5)=CC=C34)=N2)C=C1)NC6=NOC(C)(C)C)=C6

Ikhodi ye-InChi:

I-InChI=1S/C29H32N6O4S/c1-29(2,3)25-17-26(33-39-25)32-27(36)30-20-6-4-19(5-7-20)22- 18-35-23-9-8-21(16-24(23)40-28(35)31-22)38-15-12-34-10-13-37-14-11-34/h4- 9,16-18H,10-15H2,1-3H3,(H2,30,32,33,36)

I-InChi Key:

I-CVWXJKQAOSCOAB-UHFFFAOYSA-N

Igama elingukhiye:

I-Quizartinib, AC-010220, AC010220, AC 010220, AC-220, AC220, AC 220, 950769-58-1

Ukunyibilika:I-Soluble ku-DMSO

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

Incazelo:

I-Quizartinib iyi-inhibitor ye-FMS ehlobene ne-tyrosine kinase 3 (FLT3; Kd = 1.6 nM) futhi ibonisa ukukhetha okuphezulu kwe-FLT3 uma ihlolwe ngokumelene nephaneli ye-227 kinases eyengeziwe. Ivimbela ukwanda komugqa womuntu we-leukemia cell MV4-11, ephethe ukuguqulwa kwe-homozygous FLT3-ITD, enenani le-IC50 elingu-0.56 nM.1 Ku-1 mg/kg/ngosuku, i-quizartinib ikhonjiswe ukuthi yandisa ukuphila egundwaneni. imodeli ye-FLT3-ITD acute myeloid leukemia kanye nokuqeda izimila kumodeli ye-xenograft yegundane elincike ku-FLT3 ngo-10 mg/kg.

Ithagethi: FLT3