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

FLT3-IN-3 

Cat. No.: HY-112145
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

Size Stock
100 mg Get quote
250 mg Get quote
500 mg Get quote

* Please select Quantity before adding items.

Top Publications Citing Use of Products
  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

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].

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].

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.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
FLT3-IN-3
Cat. No.:
HY-112145
Quantity:

FLT3-IN-3

Cat. No.: HY-112145