2. Protein Tyrosine Kinase/RTK JAK/STAT Signaling Epigenetics Stem Cell/Wnt
  3. FLT3 JAK c-Kit
  4. JI6

JI6 是一种有效，选择性和具有口服活性的 FLT3 抑制剂，抑制 FLT3-WT，FLT3-D835Y 和 FLT3-D835H 的 IC50 值分别为 ~40，8 和 4 nM。JI6 还抑制 JAK3 和 c-Kit，IC50 值分别为 ~250 和 ~500 nM。JI6 可用于急性髓性白血病的研究。

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JI6 Chemical Structure

JI6 Chemical Structure

CAS No. : 856436-16-3

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规格 价格 是否有货 数量
1 mg ￥1952
1 周
5 mg   询价  
10 mg   询价  

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JI6 相关抗体

Top Publications Citing Use of Products

查看 JAK 亚型特异性产品:

查看所有亚型
JAK1 JAK2 JAK3 Tyk2 JAK

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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, with IC50s 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]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

JI6 相关抗体:

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]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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
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.
纯度 & 产品资料
参考文献

JI6 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

JI6856436-16-3JI 6JI-6FLT3JAKc-KitCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Janus kinaseSCFRCD117acute myeloid leukemiaAMLInhibitorinhibitorinhibit

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