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JI6
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
JI6图片
CAS NO:856436-16-3
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
JI6 是一种有效,选择性和具有口服活性的FLT3抑制剂,抑制FLT3-WTFLT3-D835YFLT3-D835HIC50值分别为 ~40,8 和 4 nM。JI6 还抑制JAK3c-KitIC50值分别为 ~250 和 ~500 nM。JI6 可用于急性髓性白血病的研究。
生物活性

JI6 is a potent, selective and orally activeFLT3inhibitor, withIC50s of ~40, 8, and 4 nM forFLT3-WT,FLT3-D835Y, andFLT3-D835H, respectively. JI6 also inhibitsJAK3andc-Kit, withIC50s of ~250 and ~500 nM, respectively. JI6 can be used for the research of acute myeloid leukemia[1].

IC50& Target[1]

FLT3-D835H

4 nM (IC50)

FLT3-D835Y

8 nM (IC50)

FLT3-WT

40 nM (IC50)

JAK3

~250 nM (IC50)

c-Kit

~500 nM (IC50)

体外研究
(In Vitro)

JI6 (3-1000 nM; 1-4 days) 以剂量依赖性方式抑制 MV4-11 细胞的活力,IC50值为 ~25 nM[1]
JI6 (1-2000 nM; 48 h) 有效抑制表达 FLT3-ITD,FLT3-D835Y 和 FLT3-D835H 的 HCD-57 细胞的活力,IC50值为 ~40 nM,对亲代 HCD-57 或表达 JAK2V617F 的细胞基本没有影响[1]
JI6 (100-500 nM; 24 h) 在表达 FLT3-ITD 和 FLT3-D835Y 的 HCD-57 细胞中诱导细胞凋亡和细胞周期停滞[1]
JI6 (50-500 nM; 3 h) 抑制表达 FLT3-ITD 和 FLT3-D835Y 的 HCD-57 细胞中 FLT3 及 ERK 和 Akt 的磷酸化[1]

Cell Viability Assay[1]

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[1]

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[1]

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[1]

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.
体内研究
(In Vivo)

JI6 (15 mg/kg; i.p. daily for 3 weeks) 抑制免疫缺陷小鼠体内表达 FLT3-D835Y 的 HCD-57 增殖并延长小鼠存活期[1]
JI6 (25 mg/kg; p.o. daily for 3 weeks) 抑制 FLT3-ITD 敲入小鼠的骨髓增生表型[1]
JI6 (100 mg/kg; a single i.p.) 在表达 FLT3-D835Y 的小鼠中显着抑制 FLT3 磷酸化和下游信号转导[1]

Animal Model:NSG mice (10-12 weeks old, male) were implanted with FLT3-D835Y-transformed HCD-57 cells[1]
Dosage:15 mg/kg
Administration:I.p. daily for 3 weeks
Result:Reduced the spleen size and prolonged the survival of these mice.
分子量

383.42

Formula

C19H17N3O4S

CAS 号

856436-16-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.