Art. -Nr.: HY-12333

Denfivontinib

(Synonyms: G-749)

2 Cited Publications

Kundenbewertung

Based on 2 publication(s) in Google Scholar

Denfivontinib (G-749) is a potent, oral active and ATP competitive FLT3 inhibitor, with IC₅₀s of 0.4 nM and 0.6 nM for FLT3 wild type and FLT3-D835Y, respectively. Denfivontinib can be used for the research of agent resistance for acute myeloid leukemia (AML).

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Reinheit: 98.0%
CAS. Nr.: 1457983-28-6
Formel: C₂₅H₂₅BrN₆O₂
Molecular Weight:521.41

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Denfivontinib Chemical Structure

CAS. Nr.: 1457983-28-6

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (2)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC50: 0.4 nM (FLT3-WT), 0.6 nM (FLT3-D835Y)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	21.4 nM Compound: G-749	Antiproliferative activity against mouse BaF3 FLT3-ITD N676D cells assessed as reduction in cell viability measured after 72 hrs by MTS assay Antiproliferative activity against mouse BaF3 FLT3-ITD N676D cells assessed as reduction in cell viability measured after 72 hrs by MTS assay	[PMID: 32659083]
BaF3	IC₅₀	38.1 nM Compound: G-749	Antiproliferative activity against mouse BaF3 FLT3-ITD F691L cells assessed as reduction in cell viability measured after 72 hrs by MTS assay Antiproliferative activity against mouse BaF3 FLT3-ITD F691L cells assessed as reduction in cell viability measured after 72 hrs by MTS assay	[PMID: 32659083]
MOLM-14	IC₅₀	7.5 nM Compound: G-749	Antiproliferative activity against human MOLM-14 cells expressing FLT3-ITD mutant assessed as inhibition of cell proliferation measured after 72 hrs by celltiter-glo luminescent cell viability assay Antiproliferative activity against human MOLM-14 cells expressing FLT3-ITD mutant assessed as inhibition of cell proliferation measured after 72 hrs by celltiter-glo luminescent cell viability assay	[PMID: 32659083]
MV4-11	IC₅₀	3.5 nM Compound: G-749	Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability after 48 hrs by Alamar Blue assay Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability after 48 hrs by Alamar Blue assay	[PMID: 32659083]

In Vitro

Denfivontinib shows potent and sustained inhibition of the FLT3 wild type and mutants including FLT3-ITD, FLT3-D835Y, FLT3-ITD/N676D, and FLT3-ITD/F691L in cellular assays^[1].
Denfivontinib inhibits autophosphorylation of FLT3 with an IC₅₀ value of ≤8 nM in FLT3-WT bearing RS4-11 and in FLT3-ITD harboring MV4-11 and Molm-14 cells^[1].
Denfivontinib (0.0001-10 nM; 72 hours) shows strong antiproliferation of leukemia cells addicted to FLT3-ITD (MV4-11 and Molm-14) in a dose-dependent manner^[1].
Denfivontinib (25-100 nM; 36 hours) causes antiproliferative activity through apoptosis^[1].
Denfivontinib (1.6-1000 nM; 2 hours) shows more potent inhibition of p-FLT3, p-ERK1/2, and p-AKT than AC220 and PKC412^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

MV4-11 cells, Molm-14 cells, K562 cells, HEL cells, RS4-11 cells
Concentration:

0.0001-10 nM
Incubation Time:

72 hours
Result:

Had antiproliferative activity for leukemia cells addicted to FLT3-ITD.

Apoptosis Analysis^[1]

Cell Line:

MV4-11 cells
Concentration:

25 nM, 50 nM, 100 nM
Incubation Time:

36 hours
Result:

Increased apoptosis of MV4-11 cells in a dose-dependent manner.

Western Blot Analysis^[1]

Cell Line:

Molm-14 cells
Concentration:

1.6 nM, 80 nM, 40 nM, 200 nM, 1000 nM
Incubation Time:

2 hours
Result:

Inhibited the phosphorylation of downstream effectors in the FLT3 signaling pathway, such as p-STAT5, p-AKT, p-ERK1/2, and p-FoxO3a.

In Vivo

Denfivontinib (3-30 mg/kg; p.o.; daily; for 28 days) shows effective antitumor activity in mouse models^[1].

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

Animal Model:

Athymic nu/nu mice, subcutaneous MV4-11 xenograft mice^[1]
Dosage:

3 mg/kg, 10 mg/kg, 30 mg/kg
Administration:

Oral administration, daily, for 28 days
Result:

Suppressed tumor growth.

Chemical Information

CAS. Nr. 1457983-28-6
Appearance Solid
Molecular Weight 521.41
Formel C₂₅H₂₅BrN₆O₂
Color White to off-white
SMILES

O=C1NC=C(C2=C1C(NC3=CC=C(C=C3)OC4=CC=CC=C4)=NC(NC5CCN(CC5)C)=N2)Br
Synonyms

G-749
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (2)

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Adv Sci (Weinh)

NAT10 Increases Lysosomal Acidification to Promote Esophageal Cancer Metastasis via ac4C Acetylation of ATP6V0E1 mRNA. [Abstract]

2025 Aug;12(31):e02931. PMID: 40729677
Anal Chem

Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]

2025 Jun 3;97(21):11099-11109. PMID: 40401576

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 25 mg/mL (47.95 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

1.9179 mL

9.5894 mL

19.1788 mL

5 mM

0.3836 mL

1.9179 mL

3.8358 mL

10 mM

0.1918 mL

0.9589 mL

1.9179 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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: ≥ 2.5 mg/mL (4.79 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: 2.5 mg/mL (4.79 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (4.79 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
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)
Handling Instructions (2659 KB)

Verweise

[1]. Lee HK, et al. G-749, a novel FLT3 kinase inhibitor, can overcome drug resistance for the treatment of acute myeloid leukemia. Blood. 2014 Apr 3;123(14):2209-19. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.9179 mL	9.5894 mL	19.1788 mL	47.9469 mL
	5 mM	0.3836 mL	1.9179 mL	3.8358 mL	9.5894 mL
	10 mM	0.1918 mL	0.9589 mL	1.9179 mL	4.7947 mL
	15 mM	0.1279 mL	0.6393 mL	1.2786 mL	3.1965 mL
	20 mM	0.0959 mL	0.4795 mL	0.9589 mL	2.3973 mL
	25 mM	0.0767 mL	0.3836 mL	0.7672 mL	1.9179 mL
	30 mM	0.0639 mL	0.3196 mL	0.6393 mL	1.5982 mL
	40 mM	0.0479 mL	0.2397 mL	0.4795 mL	1.1987 mL

Denfivontinib

2 Cited Publications

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Denfivontinib

Apoptosis Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Orally Active Compound Library

Anti-Blood Cancer Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Cytokine Inhibitors Library

Cell Death Library

Anti-Drug-Resistant Compound Library

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MCE Bioactive Compound Library

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Anti-Brain Cancer Compound Library

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Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

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Publications Citing Use of MedChemExpress (MCE) Denfivontinib

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Denfivontinib

Apoptosis Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Orally Active Compound Library

Anti-Blood Cancer Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Cytokine Inhibitors Library

Cell Death Library

Anti-Drug-Resistant Compound 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

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) Denfivontinib

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Denfivontinib Related Classifications

HY-12333 Related Classifications