1. Protein Tyrosine Kinase/RTK
  2. FLT3
  3. FLT3-IN-3

FLT3-IN-3 

Cat. No.: HY-112145 Purity: 99.73%
Handling Instructions

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

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

FLT3-IN-3 Chemical Structure

FLT3-IN-3 Chemical Structure

CAS No. : 2229050-90-0

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5 mg USD 400 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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]

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].

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].

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.
Molecular Weight

490.64

Formula

C₂₇H₃₈N₈O

CAS No.

2229050-90-0

SMILES

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

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 : 250 mg/mL (509.54 mM; Need ultrasonic)

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

  • 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

  • 3.

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

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

*All of the co-solvents are provided by MCE.
References

Purity: 99.73%

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Keywords:

FLT3-IN-3FLT3Cluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Inhibitorinhibitorinhibit

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FLT3-IN-3
Cat. No.:
HY-112145
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