1. Protein Tyrosine Kinase/RTK Apoptosis
  2. FLT3 Apoptosis
  3. HI042

HI042 是一种类 FMS 酪氨酸激酶 3 (FLT3) 抑制剂。HI042 对 MOLM-13 细胞的 IC50值 为 0.62 μM,对 MV4-11 细胞为 0.33 μM,对 OCI-AML3 细胞为 0.89 μM。HI042 能选择性降低 FIT3-内部串联重复突变 (FLT3-ITD) 阳性细胞系的存活率,诱导细胞凋亡 (apoptosis),干扰细胞周期进程,并降低集落形成能力。HI042 可用于急性髓系白血病 (AML) 的研究。

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HI042

HI042 Chemical Structure

CAS No. : 898168-15-5

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HI042 is a FMS-like Tyrosine Kinase 3 (FLT3) inhibitor. HI042 shows IC50 values of 0.62 μM for MOLM-13, 0.33 μM for MV4-11, and 0.89 μM for OCI-AML3 cells. HI042 selectively reduces the viability of FLT3-internal tandem duplication (FLT3-|TD) mutations-positive cell lines, induces apoptosis, disrupts cell cycle progression, and diminishes the clonogenic potential. HI042 can be used for the research of acute myeloid leukemia (AML)[1].

IC50 & Target[1]

FLT3

 

体外研究
(In Vitro)

HI042 在 24、48 和 72 小时,对 MOLM-13 细胞的 IC50 值分别为 0.88、0.52 和 0.36 μM,而对 MV4-11 细胞的 IC50 值分别为 >40、1.03 和 0.64 μM[1]
HI042 (0.3-5 μM, 7-10 days) 可降低 MOLM-13 和 MV4-11 细胞的自主集落生长[1]
HI042 (0.25-1 μM, 72 h) 可诱导 MOLM-13 和 MV4-11 细胞凋亡并造成破坏[1]
HI042(0.25-1μM,72 小时) 可诱导 MOLM-13 和 MV4-11 细胞分化[1]
HI042 (0.06-1 μM, 72 h) 与奎扎替尼 (Quizartinib) (HY-13001) (0.12-2 nM) 联合使用时,可显著降低 MOLM-13 和 MV4-11 细胞的活性[1]

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

Cell Viability Assay[1]

Cell Line: MOLM-13 and MV4-11 cells
Concentration: 0.312, 0.625, 1.25, 2.5, 5, 10, 20, and 40 μM
Incubation Time: 24, 48 and 72 h
Result: Reduced cell viability in a time- and concentration dependent manner.

Apoptosis Analysis[1]

Cell Line: MOLM-13 and MV4-11 cells
Concentration: 0.25, 0.5 1, 2 and 4 μM
Incubation Time: 72 h
Result: Increased the SubG1 cell population.
Increased PARP1 cleavage and γH2AX expression.

Cell Differentiation Assay[1]

Cell Line: MOLM-13 and MV4-11 cells
Concentration: 0.25, 0.5 and 1 μM
Incubation Time: 72 h
Result: Increased CD11b-positive cells.
Increased expression of the genes CEBPA and CEBPB.
分子量

301.32

Formula

C14H11N3O3S

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
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  • 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.

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产品名称:
HI042
目录号:
HY-175473
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