2. Protein Tyrosine Kinase/RTK Apoptosis
  3. FLT3 Apoptosis
  4. FLT3-IN-14

FLT3-IN-14 是一种有效的 FLT3 抑制剂，对 FLT3-WT 和 FLT3-ITD 的 IC50 分别为 5.6 nM 和 1.4 nM。FLT3-IN-14 降低 FLT3 (Y591) 磷酸化，将细胞周期阻滞在 G1 期，诱导细胞凋亡 (apoptosis)。

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FLT3-IN-14 Chemical Structure

FLT3-IN-14 Chemical Structure

CAS No. : 2620551-45-1

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FLT3-IN-14 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-14 is a potent FLT3 inhibitor with IC50s of 5.6 nM and 1.4 nM for FLT3-WT and FLT3-ITD. FLT3-IN-14 reduces the phosphorylation of FLT3 (Y591), induces cell cycle arrest at G1 phase and apoptosis. FLT3-IN-14 significantly reduces the tumor growth in an MV4-11 xenograft mouse model[1].

IC50 & Target

IC50: 1.4 nM (FLT-ITD), 5.6 nM (FLT3-WT)[1]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HL-60 IC50
0.608 μM
Compound: 9c
Antiproliferative activity against human HL-60 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay
Antiproliferative activity against human HL-60 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay
[PMID: 35339838]
K562 IC50
1.582 μM
Compound: 9c
Antiproliferative activity against human K562 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay
Antiproliferative activity against human K562 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay
[PMID: 35339838]
KCL-22 IC50
0.709 μM
Compound: 9c
Antiproliferative activity against human KCL-22 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay
Antiproliferative activity against human KCL-22 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay
[PMID: 35339838]
KG-1 IC50
0.265 μM
Compound: 9c
Antiproliferative activity against human KG-1 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay
Antiproliferative activity against human KG-1 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay
[PMID: 35339838]
KG-1a IC50
0.904 μM
Compound: 9c
Antiproliferative activity against human KG-1a cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay
Antiproliferative activity against human KG-1a cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay
[PMID: 35339838]
MOLM-13 IC50
0.014 μM
Compound: 9c
Antiproliferative activity against human MOLM-13 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay
Antiproliferative activity against human MOLM-13 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay
[PMID: 35339838]
MOLT-4 IC50
0.591 μM
Compound: 9c
Antiproliferative activity against human MOLT-4 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay
Antiproliferative activity against human MOLT-4 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay
[PMID: 35339838]
MV4-11 IC50
0.011 μM
Compound: 9c
Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay
Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay
[PMID: 35339838]
NOMO-1 IC50
1.541 μM
Compound: 9c
Antiproliferative activity against human NOMO-1 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay
Antiproliferative activity against human NOMO-1 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay
[PMID: 35339838]
OCI-AML2 IC50
0.519 μM
Compound: 9c
Antiproliferative activity against human OCI-AML2 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay
Antiproliferative activity against human OCI-AML2 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay
[PMID: 35339838]
PBL GI50
> 10 μM
Compound: 9c
Cytotoxicity in human PBL cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Cytotoxicity in human PBL cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
[PMID: 35339838]
PBL GI50
8.9 μM
Compound: 9c
Cytotoxicity in phyto-hematoagglutinin induced human PBL cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Cytotoxicity in phyto-hematoagglutinin induced human PBL cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
[PMID: 35339838]
THP-1 IC50
1.454 μM
Compound: 9c
Antiproliferative activity against human THP-1 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay
Antiproliferative activity against human THP-1 cells assessed as cell growth inhibition measured upto 4 hrs by CellTiter-Blue cell viability assay
[PMID: 35339838]
体外研究
(In Vitro)

FLT3-IN-14 (compound 9c) (0-10 μM; 24 hours) inhibits the proliferation of tested twelve haematological cell lines with IC50s of 0.011-1.582 μM[1].
FLT3-IN-14 (0-10 μM; 72 hours) exhibits low toxicity, with GI50 greater than 10 μM, in resting lymphocytes[1].
FLT3-IN-14 (1-50 nM; 24 and 48 hours) accumulates annexin-V positive cells in a concentration and time-dependent manner[1].
FLT3-IN-14 (25-100 nM; 24 and 48 hours) induces a significant G1 arrest in both cell lines[1].
FLT3-IN-14 (1-50 nM; 24 hours) induces the dephosphorylation of FLT3[1].

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

FLT3-IN-14 相关抗体:

Cell Proliferation Assay

Cell Line: MOLT-4 , HL-60, KG-1, KG-1a, MOLM-13, MV4-11, NOMO-1, OCI-AML2, PL-21, THP-1, K-562, KCL-22[1]
Concentration: 0-10 μM
Incubation Time: 24 hours
Result: Inhibited the proliferation of these twelve haematological cell lines with IC50s of 0.011-1.582 μM.

Cell Cytotoxicity Assay

Cell Line: PBL[1]
Concentration: 0-10 μM
Incubation Time: 72 hours
Result: Exhibited low toxicity, with GI50 greater than 10 μM, in resting lymphocytes.

Apoptosis Analysis

Cell Line: MV4-11[1]
Concentration: 1, 10 and 50 nM
Incubation Time: 24 and 48 hours
Result: Accumulated annexin-V positive cells in a concentration and time-dependent manner.

Cell Cycle Analysis

Cell Line: MOLM-13 and MV-14[1]
Concentration: 25, 50, 75 and 100 nM
Incubation Time: 24 and 48 hours
Result: Induced a significant G1 arrest in both cell lines.

Western Blot Analysis

Cell Line: MV-14[1]
Concentration: 1, 10 and 50 nM
Incubation Time: 24 hours
Result: Induced the dephosphorylation of FLT3.
体内研究
(In Vivo)

FLT3-IN-14 (1.0 and 3.0 mg/kg; IP; daily for 28 days) significantly reduces tumor growth in a dose-dependent manner without sign of toxicity[1].

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

Animal Model: NOD/SCID female mice (subcutaneously implanted MV4-11)[1]
Dosage: 1.0 and 3.0 mg/kg
Administration: IP; daily for 28 days
Result: Significantly reduced tumor growth by 44.1% and 55.2% at 1 and 3 mg/kg, respectively.
分子量

472.56

Formula

C25H24N6O2S
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-14 相关分类

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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.

Keywords:

FLT3-IN-142620551-45-1FLT3ApoptosisCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Acute myeloid leukemiaPhosphorylationCell cytotoxicityMOLM-13MV-14NOD/SCID female miceInhibitorinhibitorinhibit

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