1. JAK/STAT Signaling Stem Cell/Wnt Apoptosis
  2. STAT Apoptosis
  3. Erasin

Erasin is a potent Erlotinib (HY-50896)-resistance antagonizing STAT3 inhibitor with IC50s of 9.7 and 24 μM against STAT3 and STAT1, respectively. Erasin induces cancer cells apoptosis.

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

Erasin Chemical Structure

Erasin Chemical Structure

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 99 In-stock
Solution
10 mM * 1 mL in DMSO USD 99 In-stock
Solid
5 mg USD 90 In-stock
10 mg USD 150 In-stock
25 mg USD 300 In-stock
50 mg USD 480 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

Erasin is a potent Erlotinib (HY-50896)-resistance antagonizing STAT3 inhibitor with IC50s of 9.7 and 24 μM against STAT3 and STAT1, respectively. Erasin induces cancer cells apoptosis[1].

IC50 & Target[1]

STAT3

9.7 μM (IC50)

STAT1

24 μM (IC50)

In Vitro

Erasin inhibits protein-protein interactions mediated by STAT SH2 domains[1].
Erasin (0-80 μM; 24 h) induces apoptosis in MDA-MB-231, HCC-827 and Erlotinib (HY-50896)-resistant HCC-827 cells[1].

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

Western Blot Analysis[1]

Cell Line: HepG2 and K562 cells
Concentration: 0, 5, 10, 25, 50 and 100 μM
Incubation Time: 24 h (pretreated for 1-2h)
Result: Inhibited interleukin (IL)-6-stimulated STAT3 Tyr705 phosphorylation in HepG2 cells in a dose-dependent manner. Interferon (IFN)-γ-stimulated phosphorylation of STAT1 Tyr701 was inhibited to a lesser extent. Tyrosine phosphorylation of STAT5 in K562 cells was not inhibited.

Apoptosis Analysis[1]

Cell Line: MDA-MB-231, HCC-827, Erlotinib (HY-50896)-resistant HCC-827 and MDA-MB-453 cells
Concentration: 0, 20, 40, 60 and 80 μM
Incubation Time: 24 h
Result: Induced a dose-dependent increase in the rate of apoptosis in MDA-MB-231 and HCC-827 cells, compared to DMSO-treated control cells. Was equally effective at increasing the apoptotic rate of Erlotinib-resistant HCC-827 cells and parental HCC-827 cells compared to the respective DMSO-treated control cells.

Western Blot Analysis[1]

Cell Line: Parental HCC-827 cells and Erlotinib (HY-50896)-resistant HCC-827 cells
Concentration: 0, 20, 40, 60 and 80 μM
Incubation Time: 24 h (pretreated for 1-2h)
Result: Showed a dose-dependent inhibitory effect on STAT3 Tyr705 phosphorylation in both parental HCC-827 and Erlotinib-resistant HCC-827 cells.
Molecular Weight

349.38

Formula

C20H19N3O3

Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(N/N=C/C1=COC(C=CC(C(C)(C)C)=C2)=C2C1=O)C3=CC=CN=C3

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 : 35 mg/mL (100.18 mM; ultrasonic and warming and heat to 60°C; 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 2.8622 mL 14.3111 mL 28.6221 mL
5 mM 0.5724 mL 2.8622 mL 5.7244 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)

Mass
=
Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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 (5.95 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 (5.95 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:

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

Purity: 96.02%

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 2.8622 mL 14.3111 mL 28.6221 mL 71.5553 mL
5 mM 0.5724 mL 2.8622 mL 5.7244 mL 14.3111 mL
10 mM 0.2862 mL 1.4311 mL 2.8622 mL 7.1555 mL
15 mM 0.1908 mL 0.9541 mL 1.9081 mL 4.7704 mL
20 mM 0.1431 mL 0.7156 mL 1.4311 mL 3.5778 mL
25 mM 0.1145 mL 0.5724 mL 1.1449 mL 2.8622 mL
30 mM 0.0954 mL 0.4770 mL 0.9541 mL 2.3852 mL
40 mM 0.0716 mL 0.3578 mL 0.7156 mL 1.7889 mL
50 mM 0.0572 mL 0.2862 mL 0.5724 mL 1.4311 mL
60 mM 0.0477 mL 0.2385 mL 0.4770 mL 1.1926 mL
80 mM 0.0358 mL 0.1789 mL 0.3578 mL 0.8944 mL
100 mM 0.0286 mL 0.1431 mL 0.2862 mL 0.7156 mL
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Erasin 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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Product Name:
Erasin
Cat. No.:
HY-115594
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