FLT3/TrKA-IN-1

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

FLT3/TrKA-IN-1 

FLT3/TrKA-IN-1 是一种有效的 FLT3/TrKA 双激酶抑制剂，FLT3、FLT3-ITD、FLT3-TKD 和 TrKA 酶的IC50 值分别为 43.8 nM、97.2 nM、92.5 nM 和 23.6 nM。FLT3/TrKA-IN-1 诱导细胞周期停滞在 G0/G1 期，细胞凋亡 (apoptosis) 和具有抗增殖活性。FLT3/TrKA-IN-1 具有研究急性髓性白血病 (AML) 的潜力。

FLT3/TrKA-IN-1

FLT3/TrKA-IN-1 Chemical Structure

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生物活性

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)[1].

IC50 & Target[1]

TrkA

23.6 nM (IC50)

FLT3

43.8 nM (IC50)

FLT3-ITD

97.2 nM (IC50)

FLT3-TKD

92.5 nM (IC50)

体外研究
(In Vitro)

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: MV4-11, MOLM-13 cells
Concentration: 1000, 2000, 3000, 4000, 5000 nM
Incubation Time: 24, 48, 72 h
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.

Western Blot Analysis[1]

Cell Line: MV4-11, MOLM-13 cells
Concentration: 0, 10, 50, 100 nM
Incubation Time: 72 h
Result: Induced cell cycle arrest at the G0/G1 phase.

Apoptosis Analysis[1]

Cell Line: MV4-11, MOLM-13 cells
Concentration: 0, 10, 50, 100 nM
Incubation Time: 72 h
Result: Induced apoptosis and necrotic cell death of FLT3-ITD harboring AML cells.

Cell Cytotoxicity Assay[1]

Cell Line: BNL, H9c2 cells
Concentration: 0, 1, 10, 100, 1000 nM
Incubation Time: 72 h
Result: Did not elicit drastic cytotoxic effects on BNL and H9c2 cells.

分子量

454.56

Formula

C28H30N4O2
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.
参考文献

  • [1]. Dokla EME, et al. Discovery of a benzimidazole-based dual FLT3/TrKA inhibitor targeting acute myeloid leukemia. Bioorg Med Chem. 2022; 56:116596.

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