您好,欢迎来到试剂仪器网! [登录] [免费注册]
试剂仪器网
位置:首页 > 产品库 > FLT3-IN-12
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
FLT3-IN-12
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-12图片
CAS NO:2499966-67-3
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-12 是一种有效的、选择性的、具有口服活性的FLT3激酶抑制剂,对FLT3-WTFLT3-D835YIC50分别为 1.48 nM 和 2.87 nM。FLT3-IN-12 具有比 c-KIT 高的选择性 (>1000 倍)。FLT3-IN-12 具有出色的抗急性髓性白血病活性 (MV4-11细胞,IC50为 0.75 nM)。
生物活性

FLT3-IN-12 is a potent, selective and orally activeFLT3kinase inhibitor withIC50s of 1.48 nM and 2.87 nM forFLT3-WTandFLT3-D835Y, respectively. FLT3-IN-12 possesses high selectivity overc-KIT(>1000-fold). FLT3-IN-12 has an excellent anti-AML (acute myeloid leukemia) activity (MV4-11,IC50of 0.75 nM)[1].

IC50& Target

IC50: 1.48 nM (FLT3-WT) and 2.87 nM (FLT3-D835Y)[1]

体外研究
(In Vitro)

FLT3-IN-12 (compound 36) efficiently inhibits the growth of multiple mutant BaF3 cells expressing FLT3-ITD, FLT3-D835V/F, FLT3-F691L, FLT3-ITD-F691L, and FLT3-ITD-D835Y with the IC50range is 0.16-14.5 nM[1].

体内研究
(In Vivo)

Oral administration of FLT3-IN-12 (compound 36) at 6 mg/kg/d could significantly suppress tumor growth in the MV4-11 cell-inoculated xenograft model, exhibiting a tumor growth inhibitory rate of 95.1%. Importantly, FLT3-IN-12 could prolong the mouse survival time in the FLT3-ITD-TKD dual mutation syngeneic mouse model (BaF3-FLT3-ITD-D835Y) at a dose of 6 mg/kg p.o. bid/4W[1].
FLT3-IN-12 (compound 36; 20 mg/kg; oral administration) exhibits excellent plasma exposure (area under the curve (AUC)0–∞of 5278 ng·h/mL), T1/2of 3.7 hours, and high maximum plasma concentrations (Cmaxof 775 ng/mL)[1].

分子量

432.44

Formula

C21H23F3N6O

CAS 号

2499966-67-3

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.