FLT3-IN-14

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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)。

FLT3-IN-14

FLT3-IN-14 Chemical Structure

CAS No. : 2620551-45-1

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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]

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].

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

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].

Shanghai Jinpan Biotech Co Ltd 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

2620551-45-1

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]. Cilibrasi V, Spanò V, Bortolozzi R, et al. Synthesis of 2H-Imidazo[2′,1′:2,3] [1,3]thiazolo[4,5-e]isoindol-8-yl-phenylureas with promising therapeutic features for the treatment of acute myeloid leukemia (AML) with FLT3/ITD mutations. Eur J Med Chem. 2022;235:114292.

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