FLT3/TrKA-IN-1
FLT3/TrKA-IN-1 is a potent FLT3/TrKA dual kinase inhibitor with the IC50s of 43.8 nM, 97.2 nM, 92.5 nM and 23.6 nM for FLT3, FLT3-ITD, FLT3-TKD and TrKA, respectively. FLT3/TrKA-IN-1 induces cell cycle arrest at the G0/G1 phase as well as apoptosis and shows antiproliferative activity in vitro. FLT3/TrKA-IN-1 has the potential for the research of Acute myeloid leukemia (AML).
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- 分子式: C28H30N4O2
- 分子量:454.56
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
|
TrkA 23.6 nM (IC50) |
FLT3 43.8 nM (IC50) |
FLT3-ITD 97.2 nM (IC50) |
FLT3-TKD 92.5 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| KM12 | IC50 |
358 nM
Compound: 4ACP
|
Anticancer activity against human KM12 cells assessed as cell viability after 72 hrs by ATP Cell Titer G1oTM assay
Anticancer activity against human KM12 cells assessed as cell viability after 72 hrs by ATP Cell Titer G1oTM assay
|
[PMID: 35033885] |
| MOLM-13 | IC50 |
38.8 nM
Compound: 4ACP
|
Anticancer activity against human MOLM-13 cells expressing heterogenous AML-FLT3-ITD assessed as cell viability after 72 hrs by ATP Cell Titer G1oTM assay
Anticancer activity against human MOLM-13 cells expressing heterogenous AML-FLT3-ITD assessed as cell viability after 72 hrs by ATP Cell Titer G1oTM assay
|
[PMID: 35033885] |
| MV4-11 | IC50 |
54.9 nM
Compound: 4ACP
|
Anticancer activity against human MV4-11 cells expressing homozygous AML-FLT3-ITD assessed as cell viability after 72 hrs by ATP Cell Titer G1oTM assay
Anticancer activity against human MV4-11 cells expressing homozygous AML-FLT3-ITD assessed as cell viability after 72 hrs by ATP Cell Titer G1oTM assay
|
[PMID: 35033885] |
FLT3/TrKA-IN-1 (compound 4ACP) (1000, 2000, 3000, 4000, 5000 nM; 24, 48, 72 h) shows antiproliferative activity in a concentration and time-dependent pattera with IC50s of 38.8 nM, 54.9 nM for MOLM-13 and MV4-11 cells, respectively[1].
FLT3/TrKA-IN-1 (500, 1000, 1500, 2000, 2500 nM) dose not elicit cytotoxic activity against GDM-1 and THP-1 AML cell lines which do not carry FLT3-ITD mutation[1].
FLT3/TrKA-IN-1 shows potent activity against colon cancer KM12 cell line with an GI50 value of 358 nM[1].
FLT3/TrKA-IN-1 (0, 10, 50, 100 nM; 24 h, 48 h) inhibits ERK1/2 (extracellular regulated kinases 1/2) and mTOR (mammalian target of rapamycin) in FLT3-ITD positive AML (acute myeloid leukemia) cell lines in a dose-dependent manner[1].
FLT3/TrKA-IN-1 (0, 10, 50, 100 nM; 72 h) induces cell cycle arrest at the G0/G1 phase as well as apoptosis and necrotic cell death of FLT3-ITD harboring AML cells[1].
FLT3/TrKA-IN-1 ( 0, 1, 10, 100, 1000 nM; 72 h) dose not elicit drastic cytotoxic effects on BNL and H9c2 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MV4-11, MOLM-13 cells
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Concentration:1000, 2000, 3000, 4000, 5000 nM
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Incubation Time:24, 48, 72 h
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Result:Showed antiproliferative activity in a concentration and time-dependent pattera with IC50s of 38.8 nM, 54.9 nM for MOLM-13 and MV4-11 cells, respectively.
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Cell Line:MV4-11, MOLM-13 cells
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Concentration:0, 10, 50, 100 nM
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Incubation Time:72 h
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Result:Induced cell cycle arrest at the G0/G1 phase.
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Cell Line:MV4-11, MOLM-13 cells
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Concentration:0, 10, 50, 100 nM
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Incubation Time:72 h
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Result:Induced apoptosis and necrotic cell death of FLT3-ITD harboring AML cells.
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Cell Line:BNL, H9c2 cells
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Concentration:0, 1, 10, 100, 1000 nM
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Incubation Time:72 h
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Result:Did not elicit drastic cytotoxic effects on BNL and H9c2 cells.
化学情報
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分子量 454.56
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分子式 C28H30N4O2
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SMILES
CC(NC1=CC=C(C=C1)N2C=NC3=CC(C4=CC=C(C=C4)OCCN5CCCCC5)=CC=C32)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)