2. Protein Tyrosine Kinase/RTK
    Apoptosis
  3. FLT3
    Apoptosis
  4. Denfivontinib

Denfivontinib  (Synonyms: G-749)

Cat. No.: HY-12333 Purity: 98.30%
COA Handling Instructions

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).

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

Denfivontinib Chemical Structure

Denfivontinib Chemical Structure

CAS No. : 1457983-28-6

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Solution
10 mM * 1 mL in DMSO USD 109 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 109 In-stock
Solid
1 mg USD 50 In-stock
5 mg USD 95 In-stock
10 mg USD 165 In-stock
25 mg USD 375 In-stock
50 mg USD 638 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

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)[1].

IC50 & Target

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

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].

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.
Molecular Weight

521.41

Appearance

Solid

Formula

C25H25BrN6O2
CAS No.
SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (47.95 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
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.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 98.30%

COA (254 KB) LCMS (100 KB)

Handling Instructions (2659 KB)
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

Denfivontinib1457983-28-6G-749G749G 749FLT3ApoptosisCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Fms-liketyrosinereceptorkinaseacutemyeloidleukemiaAMLdrugresistanceInhibitorinhibitorinhibit

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