FLT3-IN-14

发表于由

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-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

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

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.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

发表回复