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

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 Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 363 In-stock
Solution
10 mM * 1 mL in DMSO USD 363 In-stock
Solid
5 mg USD 330 In-stock
10 mg USD 550 In-stock
25 mg USD 1012 In-stock
50 mg USD 1430 In-stock
100 mg USD 2255 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

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].

MedChemExpress (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].

MedChemExpress (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.
Appearance

Solid

Color

White to off-white

SMILES

N[C@H](CC1)CC[C@@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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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mg/kg

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.73%

References

Complete Stock Solution Preparation Table

* 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0382 mL 10.1908 mL 20.3815 mL 50.9539 mL
5 mM 0.4076 mL 2.0382 mL 4.0763 mL 10.1908 mL
10 mM 0.2038 mL 1.0191 mL 2.0382 mL 5.0954 mL
15 mM 0.1359 mL 0.6794 mL 1.3588 mL 3.3969 mL
20 mM 0.1019 mL 0.5095 mL 1.0191 mL 2.5477 mL
25 mM 0.0815 mL 0.4076 mL 0.8153 mL 2.0382 mL
30 mM 0.0679 mL 0.3397 mL 0.6794 mL 1.6985 mL
40 mM 0.0510 mL 0.2548 mL 0.5095 mL 1.2738 mL
50 mM 0.0408 mL 0.2038 mL 0.4076 mL 1.0191 mL
60 mM 0.0340 mL 0.1698 mL 0.3397 mL 0.8492 mL
80 mM 0.0255 mL 0.1274 mL 0.2548 mL 0.6369 mL
100 mM 0.0204 mL 0.1019 mL 0.2038 mL 0.5095 mL
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FLT3-IN-3 Related Classifications

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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