1. Protein Tyrosine Kinase/RTK
  2. FLT3
  3. FLT3/D835Y-IN-1

FLT3/D835Y-IN-1 

Cat. No.: HY-143434
Handling Instructions

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).

For research use only. We do not sell to patients.

FLT3/D835Y-IN-1 Chemical Structure

FLT3/D835Y-IN-1 Chemical Structure

CAS No. : 2648799-49-7

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Description

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)

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].

MCE 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.
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

MCE 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.
Molecular Weight

403.43

Formula

C22H21N5O3

CAS No.
SMILES

O=C1NC2=C(C=CC=C2)/C1=C3NC4=C(C=CC=C4)C/3=N\OCC(N5CCNCC5)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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FLT3/D835Y-IN-1
Cat. No.:
HY-143434
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