Cat. No.: HY-112145

FLT3-IN-3

3 Cited Publications

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Based on 3 publication(s) in Google Scholar

FLT3-IN-3 is a potent FLT3 inhibitor with IC₅₀s of 13 and 8 nM for FLT3 WT and FLT3 D835Y, respectively.

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Pureté: 99.95%
CAS No.: 2229050-90-0
Formule: C₂₇H₃₈N₈O
Masse moléculaire:490.64

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

FLT3-IN-3 Chemical Structure

CAS No.: 2229050-90-0

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (3)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

FLT3-IN-3 is a potent FLT3 inhibitor with IC₅₀s of 13 and 8 nM for FLT3 WT and FLT3 D835Y, respectively.

IC₅₀ & Target

IC50: 13 nM (FLT3 WT), 8 nM (FLT3 D835Y)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	GI₅₀	1.136 μM Compound: 7d	Growth inhibition of mouse BA/F3 cells after 72 hrs by calcein AM dye-based fluorescence assay Growth inhibition of mouse BA/F3 cells after 72 hrs by calcein AM dye-based fluorescence assay	[PMID: 29672049]
BJ	GI₅₀	12.343 μM Compound: 14q	Cytotoxicity against human BJ cells assessed as growth inhibition after 72 hrs by resazurin dye-based fluorescence analysis Cytotoxicity against human BJ cells assessed as growth inhibition after 72 hrs by resazurin dye-based fluorescence analysis	[PMID: 31514019]
BJ	GI₅₀	12.663 μM Compound: 7d	Growth inhibition of human BJ cells after 72 hrs by calcein AM dye-based fluorescence assay Growth inhibition of human BJ cells after 72 hrs by calcein AM dye-based fluorescence assay	[PMID: 29672049]
CCRF-CEM	GI₅₀	0.82 μM Compound: 14q	Cytotoxicity against human CEM cells assessed as growth inhibition after 72 hrs by resazurin dye-based fluorescence analysis Cytotoxicity against human CEM cells assessed as growth inhibition after 72 hrs by resazurin dye-based fluorescence analysis	[PMID: 31514019]
EOL1	GI₅₀	0.007 μM Compound: 14q	Cytotoxicity against FIP1L1-PDGFRA positive human EOL-1 cells assessed as growth inhibition after 72 hrs by resazurin dye-based fluorescence analysis Cytotoxicity against FIP1L1-PDGFRA positive human EOL-1 cells assessed as growth inhibition after 72 hrs by resazurin dye-based fluorescence analysis	[PMID: 31514019]
HCC827	GI₅₀	0.327 μM Compound: 7d	Growth inhibition of human HCC827 cells after 72 hrs by calcein AM dye-based fluorescence assay Growth inhibition of human HCC827 cells after 72 hrs by calcein AM dye-based fluorescence assay	[PMID: 29672049]
HCC827	GI₅₀	1.011 μM Compound: 14q	Cytotoxicity against human HCC827 cells assessed as growth inhibition after 72 hrs by resazurin dye-based fluorescence analysis Cytotoxicity against human HCC827 cells assessed as growth inhibition after 72 hrs by resazurin dye-based fluorescence analysis	[PMID: 31514019]
HUVEC	GI₅₀	5.866 μM Compound: 7d	Growth inhibition of HUVEC after 72 hrs by calcein AM dye-based fluorescence assay Growth inhibition of HUVEC after 72 hrs by calcein AM dye-based fluorescence assay	[PMID: 29672049]
K562	GI₅₀	0.38 μM Compound: 7d	Growth inhibition of human K562 cells after 72 hrs by calcein AM dye-based fluorescence assay Growth inhibition of human K562 cells after 72 hrs by calcein AM dye-based fluorescence assay	[PMID: 29672049]
K562	GI₅₀	1.121 μM Compound: 14q	Cytotoxicity against human K562 cells assessed as growth inhibition after 72 hrs by resazurin dye-based fluorescence analysis Cytotoxicity against human K562 cells assessed as growth inhibition after 72 hrs by resazurin dye-based fluorescence analysis	[PMID: 31514019]
Kasumi 1	GI₅₀	0.513 μM Compound: 7d	Growth inhibition of human Kasumi-1 cells after 72 hrs by calcein AM dye-based fluorescence assay Growth inhibition of human Kasumi-1 cells after 72 hrs by calcein AM dye-based fluorescence assay	[PMID: 29672049]
MCF7	GI₅₀	0.197 μM Compound: 7d	Growth inhibition of human MCF7 cells after 72 hrs by calcein AM dye-based fluorescence assay Growth inhibition of human MCF7 cells after 72 hrs by calcein AM dye-based fluorescence assay	[PMID: 29672049]
MOLM-13	GI₅₀	0.001 μM Compound: 7d	Growth inhibition of human MOLM13 cells after 72 hrs by calcein AM dye-based fluorescence assay Growth inhibition of human MOLM13 cells after 72 hrs by calcein AM dye-based fluorescence assay	[PMID: 29672049]
MRC5	GI₅₀	20.565 μM Compound: 7d	Growth inhibition of human MRC5 cells after 72 hrs by calcein AM dye-based fluorescence assay Growth inhibition of human MRC5 cells after 72 hrs by calcein AM dye-based fluorescence assay	[PMID: 29672049]
MV4-11	GI₅₀	0.002 μM Compound: 7d	Growth inhibition of human MV4-11 cells after 72 hrs by calcein AM dye-based fluorescence assay Growth inhibition of human MV4-11 cells after 72 hrs by calcein AM dye-based fluorescence assay	[PMID: 29672049]
Sf9	IC₅₀	0.027 μM Compound: 14q	Inhibition of recombinant human 3C cleavage site/N-terminal GST-His6 fused PDGFR alpha C-terminal fragment (Q551 to L1089 residues) harboring V561D mutant expressed in baculovirus infected Sf9 insect cells using AGLT peptide as substrate in presence of [g Inhibition of recombinant human 3C cleavage site/N-terminal GST-His6 fused PDGFR alpha C-terminal fragment (Q551 to L1089 residues) harboring V561D mutant expressed in baculovirus infected Sf9 insect cells using AGLT peptide as substrate in presence of [g	[PMID: 31514019]
THP-1	GI₅₀	0.713 μM Compound: 7d	Growth inhibition of human THP1 cells after 72 hrs by calcein AM dye-based fluorescence assay Growth inhibition of human THP1 cells after 72 hrs by calcein AM dye-based fluorescence assay	[PMID: 29672049]
U-937	GI₅₀	0.664 μM Compound: 7d	Growth inhibition of human U937 cells after 72 hrs by calcein AM dye-based fluorescence assay Growth inhibition of human U937 cells after 72 hrs by calcein AM dye-based fluorescence assay	[PMID: 29672049]

In Vitro

FLT3-IN-3 (Compound 7d) inhibits the proliferation of FLT3-ITD positive MV4-11 and MOLM-13 cell lines very effectively at low nanomolar concentrations (GI₅₀ values 2 and 1 nM, respectively)^[1].
FLT3-IN-3 (1 nM, 10nM, 100 nM, 1 μM and 10 μM; 72 hours) inhibits the Ba/F3 FLT3-ITD cells with the GI₅₀ of 0.034±0.015 μM, and inhibits the parental Ba/F3 cells with the GI₅₀ value of 1.136±0.389 μM^[1].
Concentrations as low as 1 nM are sufficient to block the autophosphorylation of the FLT3 receptor tyrosine kinase at three different tyrosine residues (589, 591, and 842). Moreover, this inhibition suppresses phosphorylation of several downstream targets of FLT3. Notably, FLT3-IN-3 (0.01, 0.1, 1, 10 and 100 nM; 1 hours) abolishes phosphorylation of STAT5 at Y694, which is a direct substrate of the oncogenic FLT3-ITD variant. The second pathway affected is the MAPK cascade: Two key components of this signaling pathway, ERK1/2 (T202/Y204) and MEK1/2 (S217/221), exhibit reduced phosphorylation upon treatment with FLT3-IN-3. FLT3-IN-3 also interfers with PI3K/AKT pathway which is confirmed by reduced phosphorylation of AKT at S473^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[1]

Cell Line:

Murine Ba/F3 FLT3-ITD and parental Ba/F3 cells
Concentration:

1 nM, 10nM, 100 nM, 1 μM and 10 μM
Incubation Time:

72 hours
Result:

The GI₅₀s for Ba/F3 FLT3-ITD cells and parental Ba/F3 cells are 0.034±0.015 μM and 1.136±0.389 μM, respectively.

Western Blot Analysis^[1]

Cell Line:

MV4-11 cells
Concentration:

0.01, 0.1, 1, 10 and 100 nM
Incubation Time:

1 hours
Result:

Concentrations as low as 1 nM were sufficient to block the autophosphorylation of the FLT3 receptor tyrosine kinase at three different tyrosine residues (589, 591, and 842).

In Vivo

A single dose of FLT3-IN-3 (Compound 7d; 10 mg/kg; i.p.) in mice with subcutaneous MV4-11 xenografts causes sustained inhibition of FLT3 and STAT5 phosphorylation over 48 hours^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Female athymic nu/nu mice with subcutaneously implanted MV4-11 xenografts^[1]
Dosage:

10 mg/kg
Administration:

Intraperitoneal (i.p.) injection; 48 hours
Result:

Effectively inhibited FLT3-ITD autophosphorylation in MV4-11 xenografts.

Chemical Information

CAS No. 2229050-90-0
Appearance Solid
Masse moléculaire 490.64
Formule C₂₇H₃₈N₈O
Color White to off-white
SMILES

N[C@H](CC1)CC[C@@H]1NC2=NC3=C(N=CN3C4CCCC4)C(NC5=CC=C(CN6CCOCC6)C=C5)=N2
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (3)

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EMBO J

SUCLG1 restricts POLRMT succinylation to enhance mitochondrial biogenesis and leukemia progression. [Abstract]

2024 Jun;43(12):2337-2367. PMID: 38649537
Cell Mol Gastroenterol Hepatol

Sorafenib Promotes Treg Cell Differentiation To Compromise Its Efficacy via VEGFR/AKT/Foxo1 Signaling in Hepatocellular Carcinoma. [Abstract]

2025;19(5):101454. PMID: 39743020
Bioorg Chem

Identification of FTY720 and COH29 as novel topoisomerase I catalytic inhibitors by experimental and computational studies. [Abstract]

2024 Jun:147:107412. PMID: 38696845

Solvant et solubilité

In Vitro:

DMSO : 250 mg/mL (509.54 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0382 mL

10.1908 mL

20.3815 mL

5 mM

0.4076 mL

2.0382 mL

4.0763 mL

10 mM

0.2038 mL

1.0191 mL

2.0382 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (4.24 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (4.24 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (4.24 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (283 KB)
SDS (251 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
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MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Gucký T, et al. Discovery of N2-(4-Amino-cyclohexyl)-9-cyclopentyl- N6-(4-morpholin-4-ylmethyl-phenyl)- 9H-purine-2,6-diamine as a Potent FLT3 Kinase Inhibitor for Acute Myeloid Leukemia with FLT3 Mutations. J Med Chem. 2018 May 10;61(9):3855-3869. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0382 mL	10.1908 mL	20.3815 mL	50.9539 mL
	5 mM	0.4076 mL	2.0382 mL	4.0763 mL	10.1908 mL
	10 mM	0.2038 mL	1.0191 mL	2.0382 mL	5.0954 mL
	15 mM	0.1359 mL	0.6794 mL	1.3588 mL	3.3969 mL
	20 mM	0.1019 mL	0.5095 mL	1.0191 mL	2.5477 mL
	25 mM	0.0815 mL	0.4076 mL	0.8153 mL	2.0382 mL
	30 mM	0.0679 mL	0.3397 mL	0.6794 mL	1.6985 mL
	40 mM	0.0510 mL	0.2548 mL	0.5095 mL	1.2738 mL
	50 mM	0.0408 mL	0.2038 mL	0.4076 mL	1.0191 mL
	60 mM	0.0340 mL	0.1698 mL	0.3397 mL	0.8492 mL
	80 mM	0.0255 mL	0.1274 mL	0.2548 mL	0.6369 mL
	100 mM	0.0204 mL	0.1019 mL	0.2038 mL	0.5095 mL

Keywords

FLT3-IN-3

3 Cited Publications

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FLT3-IN-3

Anti-Blood Cancer Compound Library

Membrane Protein-targeted Compound Library

Cytokine Inhibitors Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Publications Citing Use of MedChemExpress (MCE) FLT3-IN-3

Activité biologique

Chemical Information

Publications (3)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

FLT3-IN-3

Anti-Blood Cancer Compound Library

Membrane Protein-targeted Compound Library

Cytokine Inhibitors Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Publications Citing Use of MedChemExpress (MCE) FLT3-IN-3

Activité biologique

Chemical Information

Publications (3)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

FLT3-IN-3 Related Classifications

HY-112145 Related Classifications