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FLT3-IN-18
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
FLT3-IN-18图片
CAS NO:752191-77-8
包装与价格：
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
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)。
生物活性

FLT3-IN-18 is a potent and selectiveFLT3inhibitor with anIC50value of 0.003 μM. FLT3-IN-18 inducesapoptosisand cell cycle arrest at G1 phase. FLT3-IN-18 inhibitsFLT3andSTAT5phosphorylation. FLT3-IN-18 has the potential for the research of acute myeloid leukemia (AML)[1].

IC50& Target

IC50: 0.003 μM (FLT3)[1]

体外研究
(In Vitro)

FLT3-IN-18 (compound 7d) (0, 0.01, 0.1, 1, 10, 100 nM; 1h) decreases the protein 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 in MV4-11 cells[1].
FLT3-IN-18 (0, 0.01, 0.1, 1, 10, 100 nM; 24 h) induces apoptosis and cell cycle arrest at G1 phase[1].

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) effectively inhibits FLT3 and STAT5 phosphorylation in rats[1].

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

752191-77-8

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.