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FLT3/D835Y-IN-1
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/D835Y-IN-1图片
CAS NO:2648799-49-7
包装与价格：
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
FLT3/D835Y-IN-1 (化合物13a) 是一种口服有效且选择性的FLT3和FLT3/D835Y抑制剂，其IC50值分别为 0.26 nM 和 0.18 nM。FLT3/D835Y-IN-1 还能阻断肿瘤生长，具有抗癌作用，可以用于研究急性髓系白血病。
生物活性

FLT3/D835Y-IN-1 (compound 13a) is a orally active, potent and selectiveFLT3andFLT3/D835Yinhibitor, withIC50values of 0.26 nM and 0.18 nM, respectively. FLT3/D835Y-IN-1 also blocks tumor growth, has anticancer efficacy, and can be used to research for AML (acute myeloid leukemia)[1].

IC50& TargetFLT3/D835Y

FLT3/D835Y

0.18 nM (IC50)

体外研究
(In Vitro)

FLT3/D835Y-IN-1 (compound 13a) (100 nM, 3 h) potently inhibits Ba/F3-FLT3-ITD, Ba/F3-FLT3-ITD/D835Y, Ba/F3-FLT3-ITD-F691L cell lines, and AML cells proliferation[1].
FLT3/D835Y-IN-1 (3-30 nM, 16 h) significantly inhibit FLT3, AKT, ERK, and STAT5 pathways[1].

Cell Proliferation Assay

Cell Line:Ba/F3-FLT3-ITD, Ba/F3-FLT3-ITD/D835Y, and Ba/F3-FLT3-ITD-F691L cell lines, AML cells[1]
Concentration:100 nM
Incubation Time:3 h
Result:Inhibited Ba/F3-FLT3-ITD, Ba/F3-FLT3-ITD/D835Y, Ba/F3-FLT3-ITD-F691L, MV4-11, MOLM14, and MOLM14-ITD/D835Y proliferation, withGI50values of 0.59, 0.73, 5.54, 1.30, 6.20, and 4.58 nM, respectively.

Western Blot Analysis

Cell Line:MOLM14-ITD/D835Y and MOLM14-ITD/F691L cells[1].
Concentration:3, 10, and 30 nM
Incubation Time:16 h
Result:Significantly inhibited the FLT3, AKT, ERK, and STAT5 pathways at lower dosages.
体内研究
(In Vivo)

FLT3/D835Y-IN-1 (10 mg/kg, IP, daily, 6 days per week) significantly suppresses tumor growth and exhibits potent antitumor activity against MOLM14-ITD/D835Y cells[1].
FLT3/D835Y-IN-1 (10 mg/kg, IV or Orally, single) displays extremely low AUC and high clearance[1].
Pharmacokinetic Parameters of FLT3/D835Y-IN-1 in ICR mice[1].

Parameters13a
AUClast(ng*h/mL)1360 ± 110
CL (L/h/kg)6.96 ± 0.66
Vss(L/kg)14.8 ± 0.7
T1/2(h)1.5 ± 0.1

Animal Model:NOD/SCID mice (6 weeks, male, nine mice per group)[1]
Dosage:10 mg/kg
Administration:IP, daily, 6 days per week, from day 7 to day 29
Result:Significantly suppressed tumor growth.
Animal Model:ICR mice (7–8 weeks, male)[1]
Dosage:10 mg/kg, dissolved in a solution (10% DMSO, 40% PEG400, and 50% PBS)
Administration:IV or Orally, single (Pharmacokinetic Analysis)
Result:Displayed extremely low AUC and high clearance.
分子量

403.43

Formula

C22H21N5O3

CAS 号

2648799-49-7

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.