1. Protein Tyrosine Kinase/RTK
    Apoptosis
  2. FLT3
    Apoptosis
  3. G-749

G-749 

Cat. No.: HY-12333 Purity: 98.43%
Handling Instructions

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. G-749 can be used for the research of drug resistance for acute myeloid leukemia (AML).

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

G-749 Chemical Structure

G-749 Chemical Structure

CAS No. : 1457983-28-6

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 109 In-stock
Estimated Time of Arrival: December 31
1 mg USD 50 In-stock
Estimated Time of Arrival: December 31
5 mg USD 95 In-stock
Estimated Time of Arrival: December 31
10 mg USD 165 In-stock
Estimated Time of Arrival: December 31
25 mg USD 375 In-stock
Estimated Time of Arrival: December 31
50 mg USD 638 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

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Description

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. G-749 can be used for the research of drug resistance for acute myeloid leukemia (AML)[1].

IC50 & Target

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

In Vitro

G-749 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].
G-749 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].
G-749 (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].
G-749 (25-100 nM; 36 hours) causes antiproliferative activity through apoptosis[1].
G-749 (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

G-749 (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

Formula

C₂₅H₂₅BrN₆O₂

CAS No.

1457983-28-6

SMILES

O=C1C2=C(N=C(NC3CCN(C)CC3)N=C2NC4=CC=C(OC5=CC=CC=C5)C=C4)C(Br)=CN1

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 provided by MCE.
References

Purity: 98.43%

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Keywords:

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

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G-749
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