JI6

Research use only, not for human use.

JI6 (JAK3 Inhibitor VI) is a potent, selective and orally active FLT3 inhibitor. JI6 exhibits IC50s of ～40, 8, and 4 nM for FLT3-WT, FLT3-D835Y, and FLT3-D835H, respectively.

JI6 is a potent, selective and orally active FLT3 inhibitor, with IC50s of ～40, 8, and 4 nM for FLT3-WT, FLT3-D835Y, and FLT3-D835H, respectively. JI6 also inhibits JAK3 and c-Kit, withIC50s of ～250 and ～500 nM, respectively. JI6 can be used for the research of acute myeloid leukemia.

Cell Viability Assay Cell Line:MV4-11, HL60, Karpas 299, and Jurkat cells Concentration:3-1000 nM Incubation Time:48 hours Result:Inhibited MV4-11 cells and no effects of JI6 on the three remaining cells at a concentration as high as 1 μM.Apoptosis Analysis Cell Line:FLT3-ITD- and FLT3-D835Y-transformed HCD-57 cells Concentration:100, 500 nM Incubation Time:24 hours Result:Increased the percentage of apoptotic and necrotic cells and displayed no effects on the apoptosis of the parent HCD-57 cells.Cell Cycle Analysis Cell Line:FLT3-ITD- and FLT3-D835Y-transformed HCD-57 cells Concentration:100, 500 nM Incubation Time:24 hours Result:Significantly reduced G2 and S phase cells and increased G1 phase cells in both FLT3-ITD and D835Y cells.Cell Viability Assay Cell Line:FLT3-ITD- and FLT3-D835Y-transformed HCD-57 cells Concentration:50, 100, 500 nM Incubation Time:3 hours Result:Inhibited phosphorylation of FLT3, ERK1, ERK2 and Akt.

Animal Model:NSG mice (10-12 weeks old, male) were implanted with FLT3-D835Y-transformed HCD-57 cells Dosage:15 mg/kg Administration:I.p. daily for 3 weeks Result:Reduced the spleen size and prolonged the survival of these mice.

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Angiogenesis

FLT

FLT

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856436-16-3

383.42

C19H17N3O4S

>98% (HPLC)

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CS(=O)(O)=O.O=C(/C1=C\C2=CC=CN2)NC(C=C3)=C1C=C3C4=CN=CC=C4

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(-20℃)

With Ice Pack

≥ 2 years