1. Protein Tyrosine Kinase/RTK Apoptosis
  2. FLT3 c-Kit Apoptosis
  3. SKLB4771

SKLB4771  (Synonyms: FLT3-​IN-​1)

Cat. No.: HY-12960 Purity: 98.08%
COA Handling Instructions

SKLB4771 is a potent and selective Flt3 inhibitor with an IC50 value of 10 nM. SKLB4771 downregulates the phosphorylation of FLT3/STAT5/ERK, blocks cell proliferation, and induces apoptosis in tumor tissue.

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

SKLB4771 Chemical Structure

SKLB4771 Chemical Structure

CAS No. : 1370256-78-2

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 195 In-stock
Solution
10 mM * 1 mL in DMSO USD 195 In-stock
Solid
2 mg USD 110 In-stock
5 mg USD 165 In-stock
10 mg USD 250 In-stock
25 mg USD 500 In-stock
50 mg USD 800 In-stock
100 mg USD 1200 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Description

SKLB4771 is a potent and selective Flt3 inhibitor with an IC50 value of 10 nM. SKLB4771 downregulates the phosphorylation of FLT3/STAT5/ERK, blocks cell proliferation, and induces apoptosis in tumor tissue[1][2].

IC50 & Target

IC50: 10 nM (Flt3); 3.7 μM (Flt4); 1.5 μM (Aurora A); 6.8 μM (c-kit); 2.8 μM (FMS)[1]

In Vitro

SKLB4771 (compound 20c) (72 h) inhibits FLT3-ITD-expressing MV4-11 cells with an IC50 value of 6 nM, and inhibits other cancer cells with IC50s of 3.05 μM (Jurkat), 6.25 μM (Ramos), 3.72 μM (PC-9), 6.94 μM (H292), and 8.91 μM (A431), respectively[1].
SKLB4771 (0-300 nM; 20 h) inhibits FLT3 phosphorylation and also decreases the phosphorylation of the downstream signaling proteins STAT5 and ERK1/2 at concentrations >0.1 μM[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: MV4-11 cells
Concentration: 0, 30, 100, 300 nM
Incubation Time: 20 hours
Result: Resulted inhibition against the human FLT3 kinase in a dose-dependent manner, and decreased the phosphorylation level of STAT5 and ERK1/2 at 100 nM and 300 nM.
In Vivo

SKLB4771 (20-100 mg/kg; i.p.; once daily; 21 d) inhibits tumor growth in vivo without significant weight loss or any other obvious signs of toxicity on mice[1].
Pharmacokinetic Analysis of SKLB4771 in rat (40 mg/kg; i.p.)[1]

Cmax (μg/mL) T1/2 (h) AUCmax (h·μg/mL) Tmax (h) CLobs (L/h/kg)
5.31 13.9 21.86 1.0 2.21

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female NOD-SCID mouse (6−7 weeks old)[1]
Dosage: 20, 40, 100 mg/kg; dissolved in 25% (v/v) PEG400 plus 5% DMSO, administered at a dose of 5 mL/kg
Administration: Intraperitoneal injection; once daily; 21 days
Result: Inhibited tumor growth by 66% and 84% at concentration of 20 mg/kg and 40 mg/kg, respectively.
Resulted cell proliferation inhibition and apoptosis induction.
Molecular Weight

537.66

Formula

C25H27N7O3S2

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(NC1=NN=C(SC2=C3C=CC(OCCCN4CCOCC4)=CC3=NC=N2)S1)NC5=CC=C(C)C=C5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 33.33 mg/mL (61.99 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 1.8599 mL 9.2996 mL 18.5991 mL
5 mM 0.3720 mL 1.8599 mL 3.7198 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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Volume (start)

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C2

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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: ≥ 2.5 mg/mL (4.65 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: 2.5 mg/mL (4.65 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

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
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8599 mL 9.2996 mL 18.5991 mL 46.4978 mL
5 mM 0.3720 mL 1.8599 mL 3.7198 mL 9.2996 mL
10 mM 0.1860 mL 0.9300 mL 1.8599 mL 4.6498 mL
15 mM 0.1240 mL 0.6200 mL 1.2399 mL 3.0999 mL
20 mM 0.0930 mL 0.4650 mL 0.9300 mL 2.3249 mL
25 mM 0.0744 mL 0.3720 mL 0.7440 mL 1.8599 mL
30 mM 0.0620 mL 0.3100 mL 0.6200 mL 1.5499 mL
40 mM 0.0465 mL 0.2325 mL 0.4650 mL 1.1624 mL
50 mM 0.0372 mL 0.1860 mL 0.3720 mL 0.9300 mL
60 mM 0.0310 mL 0.1550 mL 0.3100 mL 0.7750 mL
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SKLB4771 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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SKLB4771
Cat. No.:
HY-12960
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