FLT3/D835Y-IN-1

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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/D835Y-IN-1 

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。

FLT3/D835Y-IN-1

FLT3/D835Y-IN-1 Chemical Structure

CAS No. : 2648799-49-7

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生物活性

FLT3/D835Y-IN-1 (compound 13a) is a orally active, potent and selective FLT3 and FLT3/D835Y inhibitor, with IC50 values 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].

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

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, with GI50 values 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].

Parameters 13a
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

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

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.
参考文献

  • [1]. Lee JH, Shin JE, Kim W, et al. Discovery of indirubin-3′-aminooxy-acetamide derivatives as potent and selective FLT3/D835Y mutant kinase inhibitors for acute myeloid leukemia. Eur J Med Chem. 2022 Apr 21;237:114356.

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