1. PROTAC Protein Tyrosine Kinase/RTK Apoptosis JAK/STAT Signaling Stem Cell/Wnt MAPK/ERK Pathway
  2. PROTACs FLT3 Apoptosis STAT MEK ERK
  3. PROTAC FLT-3 degrader 1

PROTAC FLT-3 degrader 1 is an effective and selective FLT-3 PROTAC degrader with an IC50 of 0.6 nM. PROTAC FLT-3 degrader 1 inhibits both FLT-3 and FLT-3 ITD mutants. PROTAC FLT-3 degrader 1 has the activity of anti-proliferation and induction of apoptosis, which can be used in the study of tumor. (Pink: FLT3 ligand (HY-168702); Black: Linker (HY-124380); Blue: VHL ligand (HY-125845)).

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

PROTAC FLT-3 degrader 1 Chemical Structure

PROTAC FLT-3 degrader 1 Chemical Structure

CAS No. : 2230826-81-8

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Based on 1 publication(s) in Google Scholar

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  • Purity & Documentation

  • References

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Description

PROTAC FLT-3 degrader 1 is an effective and selective FLT-3 PROTAC degrader with an IC50 of 0.6 nM. PROTAC FLT-3 degrader 1 inhibits both FLT-3 and FLT-3 ITD mutants. PROTAC FLT-3 degrader 1 has the activity of anti-proliferation and induction of apoptosis, which can be used in the study of tumor. (Pink: FLT3 ligand (HY-168702); Black: Linker (HY-124380); Blue: VHL ligand (HY-125845))[1].

IC50 & Target[1]

STAT5

 

In Vitro

PROTAC FLT-3 degrader 1 (0.05 nM-1 μM; 24 h) induces FLT-3 ITD protein degradation and inhibits downstream STAT-5, MEK and ERK phosphorylation, and has anti-proliferation and apoptosis-inducing activities in MV4-11 cells[1].

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

Cell Viability Assay[1]

Cell Line: MV4-11 cells
Concentration: 0.05, 0.5 and 2 nM
Incubation Time: 24 h
Result: Reduced the phosphorylation levels of STAT-5, MEK and ERK.
In Vivo

PROTAC FLT-3 degrader 1 (30 mg/kg; Intraperitoneal injection; 3 days) can degrade FLT-3 protein in mouse tumor model[1].
Pharmacokinetic Analysis in Mouse[1]

Route Dose (mg/kg) Cmax (ng/mL) Tmax (hr) t1/2 (hr) Plasma Protein Binding
i.p. 10 1069 2 2.31 98.0 %

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

Animal Model: MV4-11 cells treated athymic mice[1]
Dosage: 30 mg/kg
Administration: Intraperitoneal injection (i.p.); 3 days
Result: Did not cause any adverse effects.
Significantly decreased (approximately 60%) in total FLT-3 protein.
Suppressed the downstream signaling of FLT-3 ITD in tumor samples.
Molecular Weight

1020.23

Formula

C52H61N9O9S2

CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=C(N[C@@H](C(C)(C)C)C(N1[C@H](C(NCC2=CC=C(C3=C(C)N=CS3)C=C2)=O)C[C@@H](O)C1)=O)CCOCCOCCOC4=CC5=C(N6C(S5)=NC(C7=CC=C(NC(NC8=NOC(C(C)(C)C)=C8)=O)C=C7)=C6)C=C4

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 : 150 mg/mL (147.03 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 0.9802 mL 4.9009 mL 9.8017 mL
5 mM 0.1960 mL 0.9802 mL 1.9603 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

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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: 7.5 mg/mL (7.35 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 7.5 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 (75.0 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: 7.5 mg/mL (7.35 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 7.5 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 (75.0 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:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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%
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, PEG300/PEG400, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Purity & Documentation

Purity: 99.74%

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 0.9802 mL 4.9009 mL 9.8017 mL 24.5043 mL
5 mM 0.1960 mL 0.9802 mL 1.9603 mL 4.9009 mL
10 mM 0.0980 mL 0.4901 mL 0.9802 mL 2.4504 mL
15 mM 0.0653 mL 0.3267 mL 0.6534 mL 1.6336 mL
20 mM 0.0490 mL 0.2450 mL 0.4901 mL 1.2252 mL
25 mM 0.0392 mL 0.1960 mL 0.3921 mL 0.9802 mL
30 mM 0.0327 mL 0.1634 mL 0.3267 mL 0.8168 mL
40 mM 0.0245 mL 0.1225 mL 0.2450 mL 0.6126 mL
50 mM 0.0196 mL 0.0980 mL 0.1960 mL 0.4901 mL
60 mM 0.0163 mL 0.0817 mL 0.1634 mL 0.4084 mL
80 mM 0.0123 mL 0.0613 mL 0.1225 mL 0.3063 mL
100 mM 0.0098 mL 0.0490 mL 0.0980 mL 0.2450 mL
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Product Name:
PROTAC FLT-3 degrader 1
Cat. No.:
HY-114323
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