2. Protein Tyrosine Kinase/RTK
  3. FLT3
  4. FLT3-IN-18

FLT3-IN-18 是一种有效的选择性 FLT3 抑制剂，IC50 值为 0.003 μM。FLT3-IN-18 诱导细胞凋亡 (apoptosis) 和细胞周期停滞在 G1 期。FLT3-IN-18 抑制 FLT3 和 STAT5 磷酸化。FLT3-IN-18 具有研究急性髓系白血病 (AML) 的潜力。 IC50: 0.003 μM (FLT3)。

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FLT3-IN-18 Chemical Structure

FLT3-IN-18 Chemical Structure

CAS No. : 752191-77-8

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FLT3-IN-18 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

FLT3-IN-18 is a potent and selective FLT3 inhibitor with an IC50 value of 0.003 μM. FLT3-IN-18 induces apoptosis and cell cycle arrest at G1 phase. FLT3-IN-18 inhibits FLT3 and STAT5 phosphorylation. FLT3-IN-18 has the potential for the research of acute myeloid leukemia (AML)[1].

IC50 & Target

IC50: 0.003 µM (FLT3)[1]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
BJ GI50
12.249 μM
Compound: 7b
Growth inhibition of human BJ cells after 72 hrs by calcein AM dye-based fluorescence assay
Growth inhibition of human BJ cells after 72 hrs by calcein AM dye-based fluorescence assay
[PMID: 29672049]
HCC827 GI50
0.521 μM
Compound: 7b
Growth inhibition of human HCC827 cells after 72 hrs by calcein AM dye-based fluorescence assay
Growth inhibition of human HCC827 cells after 72 hrs by calcein AM dye-based fluorescence assay
[PMID: 29672049]
HUVEC GI50
4.531 μM
Compound: 7b
Growth inhibition of HUVEC after 72 hrs by calcein AM dye-based fluorescence assay
Growth inhibition of HUVEC after 72 hrs by calcein AM dye-based fluorescence assay
[PMID: 29672049]
K562 GI50
0.965 μM
Compound: 7b
Growth inhibition of human K562 cells after 72 hrs by calcein AM dye-based fluorescence assay
Growth inhibition of human K562 cells after 72 hrs by calcein AM dye-based fluorescence assay
[PMID: 29672049]
Kasumi 1 GI50
0.816 μM
Compound: 7b
Growth inhibition of human Kasumi-1 cells after 72 hrs by calcein AM dye-based fluorescence assay
Growth inhibition of human Kasumi-1 cells after 72 hrs by calcein AM dye-based fluorescence assay
[PMID: 29672049]
MCF7 GI50
0.32 μM
Compound: 7b
Growth inhibition of human MCF7 cells after 72 hrs by calcein AM dye-based fluorescence assay
Growth inhibition of human MCF7 cells after 72 hrs by calcein AM dye-based fluorescence assay
[PMID: 29672049]
MOLM-13 GI50
0.004 μM
Compound: 7b
Growth inhibition of human MOLM13 cells after 72 hrs by calcein AM dye-based fluorescence assay
Growth inhibition of human MOLM13 cells after 72 hrs by calcein AM dye-based fluorescence assay
[PMID: 29672049]
MRC5 GI50
23.265 μM
Compound: 7b
Growth inhibition of human MRC5 cells after 72 hrs by calcein AM dye-based fluorescence assay
Growth inhibition of human MRC5 cells after 72 hrs by calcein AM dye-based fluorescence assay
[PMID: 29672049]
MV4-11 GI50
0.002 μM
Compound: 7b
Growth inhibition of human MV4-11 cells after 72 hrs by calcein AM dye-based fluorescence assay
Growth inhibition of human MV4-11 cells after 72 hrs by calcein AM dye-based fluorescence assay
[PMID: 29672049]
THP-1 GI50
1.159 μM
Compound: 7b
Growth inhibition of human THP1 cells after 72 hrs by calcein AM dye-based fluorescence assay
Growth inhibition of human THP1 cells after 72 hrs by calcein AM dye-based fluorescence assay
[PMID: 29672049]
U-937 GI50
1.572 μM
Compound: 7b
Growth inhibition of human U937 cells after 72 hrs by calcein AM dye-based fluorescence assay
Growth inhibition of human U937 cells after 72 hrs by calcein AM dye-based fluorescence assay
[PMID: 29672049]
体外研究
(In Vitro)

FLT3-IN-18(compound 7d) (0, 0.01, 0.1, 1, 10, 100 nM; 1h) 在 MV4-11 细胞中呈剂量依赖性降低 p-FLT3 Y589/591，p-FLT3 Y842，p-TAT5 Y694，p-ERK1/2 T202/Y204，p-MEK1/2 S217/221，p-AKT S473 的蛋白表达[1]。
FLT3-IN-18 (0, 0.01, 0.1, 1, 10, 100 nM; 24 h) 诱导细胞凋亡和细胞周期停滞在 G1 期[1]。

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

FLT3-IN-18 相关抗体:

Cell Proliferation Assay[1]

Cell Line: MV4-11, K562, MOLM-13, Kasumi-1, THP-1, U937, MCF-7 cells
Concentration: 0-20 µM
Incubation Time: 72 h
Result: Inhibited cell growth with GI50s of 0.002, 0.380, 0.001, 0.513, 0.713, 0.664, 0.197 µM for MV4-11, K562, MOLM-13, Kasumi-1, THP-1, U937, MCF-7 cells, respectively.

Western Blot Analysis[1]

Cell Line: MV4-11 cells
Concentration: 0, 0.01, 0.1, 1, 10, 100 nM
Incubation Time: 1 h
Result: Decreased the expression of p-FLT3 Y589/591, p-FLT3 Y842, p-TAT5 Y694, p-ERK1/2 T202/Y204, and p-MEK1/2 S217/221, p-AKT S473 in a dose-dependent manner.

Cell Cycle Analysis[1]

Cell Line: MV4-11 cells
Concentration: 0, 0.01, 0.1, 1, 10, 100 nM
Incubation Time: 24 h
Result: Induced cell cycle arrest at G1 phase.

Apoptosis Analysis[1]

Cell Line: MV4-11 cells
Concentration: 0, 0.01, 0.1, 1, 10, 100 nM
Incubation Time: 24 h
Result: Increased cleavage of the apoptotic marker protein PARP-1 (89 kDa fragment) and educed levels of the antiapoptotic protein Mcl-1.
体内研究
(In Vivo)

FLT3-IN-18 (10 mg/kg; i.p.; once) 有效抑制大鼠的 FLT3 和 STAT5 磷酸化[1]。

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

Animal Model: Rats (MV4-11 xenografts)[1]
Dosage: 10 mg/kg
Administration: I.p.; once
Result: Effectively inhibited FLT3-ITD autophosphorylation in MV4-11 xenografts, reduced STAT5 phosphorylation by over 95% after 24 h.
分子量

476.62

Formula

C26H36N8O
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

FLT3-IN-18 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

FLT3-IN-18752191-77-8FLT3Cluster of differentiation antigen 135CD135Fms like tyrosine kinase 3anti-proliferativeMV4-11apoptosisG1 phasep-STAT5AMLInhibitorinhibitorinhibit

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