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FLT3/D835Y-IN-1

FLT3/D835Y-IN-1
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FLT3/D835Y-IN-1

Catalog No. T61977Cas No. 2648799-49-7
FLT3/D835Y-IN-1 (compound 13a) is a orally active, and selective inhibitor of FLT3 and FLT3/D835Y, with IC50s of 0.26 nM and 0.18 nM, respectively. FLT3/D835Y-IN-1 has anticancer efficacy, and has research value in AML (acute myeloid leukemia).
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
Pack SizePriceAvailabilityQuantity
25 mg$1,5206-8 weeks
50 mg$1,9806-8 weeks
100 mg$2,5006-8 weeks
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Product Introduction

Bioactivity
Description
FLT3/D835Y-IN-1 (compound 13a) is a orally active, and selective inhibitor of FLT3 and FLT3/D835Y, with IC50s of 0.26 nM and 0.18 nM, respectively. FLT3/D835Y-IN-1 has anticancer efficacy, and has research value in AML (acute myeloid leukemia).
In vitro
FLT3/D835Y-IN-1 (compound 13a), at a concentration of 100 nM over a period of 3 hours, effectively inhibits the proliferation of Ba/F3-FLT3-ITD, Ba/F3-FLT3-ITD/D835Y, Ba/F3-FLT3-ITD-F691L cell lines, and AML cells. When administered at concentrations ranging from 3-30 nM for 16 hours, it markedly suppresses the FLT3, AKT, ERK, and STAT5 signaling pathways. In a cell proliferation assay using these cell lines and AML cells at a 100 nM concentration and a 3-hour incubation, significant inhibition was observed alongside GI50 values of 0.59, 0.73, 5.54, 1.30, 6.20, and 4.58 nM, respectively. Additionally, Western Blot analysis of MOLM14-ITD/D835Y and MOLM14-ITD/F691L cells treated with concentrations of 3, 10, and 30 nM for 16 hours demonstrates a significant reduction in the activity of FLT3, AKT, ERK, and STAT5 pathways at lower doses.
In vivo
Administering FLT3/D835Y-IN-1 at a dosage of 10 mg/kg interperitoneally (IP) daily for six days per week notably inhibits tumor proliferation and demonstrates strong antitumor efficacy against MOLM14-ITD/D835Y cells. Conversely, administering a single dose of 10 mg/kg intravenously (IV) or orally reveals a considerably low area under the curve (AUC) and elevated clearance rates in pharmacokinetic studies, indicating rapid drug elimination. Additionally, pharmacokinetic parameters assessed in ICR mice include an AUC of 1360 ± 110 ng*h/mL, clearance rate (CL) of 6.96 ± 0.66 L/h/kg, steady-state volume of distribution (Vss) of 14.8 ± 0.7 L/kg, and a half-life (T1/2) of 1.5 ± 0.1 hours. In trials involving NOD/SCID mice (9 per group, 6 weeks old, male), the compound significantly reduced tumor size when given IP daily at 10 mg/kg from day 7 to 29. Similarly, in ICR mice (7–8 weeks old, male), a single dose of the compound, dissolved in 10% DMSO, 40% PEG400, and 50% PBS, administered IV or orally showed significantly low AUC and high clearance.
Chemical Properties
Molecular Weight403.43
FormulaC22H21N5O3
Cas No.2648799-49-7
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year

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