2. Epigenetics Stem Cell/Wnt Protein Tyrosine Kinase/RTK JAK/STAT Signaling Apoptosis Autophagy
  3. JAK STAT Apoptosis Autophagy
  4. Brevilin A

Brevilin A is an orally active STAT3/JAK inhibitor (STAT3 IC50=?10.6 μM). Brevilin A shows anti-tumor activity, anti-proliferative activity to cancer cells, and can induce apoptosis and autophagy.

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

Brevilin A Chemical Structure

Brevilin A Chemical Structure

CAS No. : 16503-32-5

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 302 In-stock
Solution
10 mM * 1 mL in DMSO USD 302 In-stock
Solid
1 mg USD 130 In-stock
5 mg USD 275 In-stock
10 mg USD 473 In-stock
25 mg USD 800 In-stock
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Customer Review

Based on 4 publication(s) in Google Scholar

Other Forms of Brevilin A:

Brevilin A Related Antibodies

Top Publications Citing Use of Products

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JAK1 JAK2 JAK3 Tyk2 JAK

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STAT3 STAT5 STAT6 STAT1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Brevilin A is an orally active STAT3/JAK inhibitor (STAT3 IC50=?10.6 μM). Brevilin A shows anti-tumor activity, anti-proliferative activity to cancer cells, and can induce apoptosis and autophagy[1][2].

IC50 & Target[1]

STAT3

10.6 μM (IC50)

Cellular Effect
Cell Line Type Value Description References
HCT-116 IC50
> 10 μM
Compound: 17
Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 33533247]
HeLa IC50
9.2 μM
Compound: 17
Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 33533247]
HepG2 IC50
> 10 μM
Compound: 17
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 33533247]
In Vitro

Brevilin A (1-20 μM; 24 h) inhibits STAT3 signaling in a dose dependent manner[1].
Brevilin A (0-50 μM; 24-72 h) inhibits the proliferation of NPC cells[2].
Brevilin A (10 μM; 24 and 48 h) induces DU145 and MDA-MB-468 apoptosis after 24 h treatment[1].
Brevilin A (12.5 and 25 μM; 24 h) blocks STAT3 tyrosine 705 phosphorylation in A549R cells[1].

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

Brevilin A Related Antibodies

Cell Viability Assay[1]

Cell Line: A549R cells
Concentration: 1-20 µM
Incubation Time: 24 hours
Result: Exhibited STAT3 signaling inhibition in a dose dependent manner with IC50 value of 10.6 µM.

Cell Proliferation Assay[2]

Cell Line: CNE-2 cells
Concentration: 0-50 μM
Incubation Time: 24, 48, and 72 hours
Result: Showed IC50 values in CNE-2 cells with treatment times of 24, 48, and 72 h of 7.93, 2.60, and 22.26 µM, respectively.

Apoptosis Analysis[1]

Cell Line: DU145 and MDA-MB-468 cells
Concentration: 10 µM
Incubation Time: 24 and 48 hours
Result: Decreased c-Myc and CyclinD1 after 24 h and 48 h treatment, increased cleaved PARP after 24 h treatment.

Western Blot Analysis[1]

Cell Line: A549R cells
Concentration: 12.5 and 25 µM
Incubation Time: 24 hours
Result: Inhibits STAT3 phosphorylation in A549R cells.
In Vivo

Brevilin A (oral gavage; 10 and 20 mg/kg; once daily; 16 d) inhibits CNE-2 xenograft tumor growth, and inhibits PI3K/AKT and STAT3 signaling in vivo[2].

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

Animal Model: Male BALB/c nude mice injected with CNE-2 cells[2]
Dosage: 10 and 20 mg/kg
Administration: Oral gavage; 10 and 20 mg/kg; once daily; 16 days
Result: Decreased average tumor volumes and weights treated with 20 mg/kg by 36.3% and 46.0%, respectively, compared to vehicle control.
Inhibited the protein expression of p-AKT and p-STAT3 at both low and high doses.
Molecular Weight

346.42

Formula

C20H26O5
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C/C=C(C)\C(O[C@H]1[C@@]([C@@H]2C)([H])[C@@](OC2=O)([H])C[C@@H](C)[C@@]3([H])[C@]1(C(C=C3)=O)C)=O
Structure Classification
Initial Source
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 : 100 mg/mL (288.67 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 2.8867 mL 14.4333 mL 28.8667 mL
5 mM 0.5773 mL 2.8867 mL 5.7733 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)

Mass
=
Concentration
×
Volume
×
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    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 10 mg/mL (28.87 mM); Clear solution

    This protocol yields a clear solution of ≥ 10 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (100.0 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 6.25 mg/mL (18.04 mM); Clear solution

    This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 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.
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: 99.81%

SDS (393 KB)

COA (255 KB) HNMR (260 KB) LCMS (88 KB)

Handling Instructions (2659 KB)
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 2.8867 mL 14.4333 mL 28.8667 mL 72.1667 mL
5 mM 0.5773 mL 2.8867 mL 5.7733 mL 14.4333 mL
10 mM 0.2887 mL 1.4433 mL 2.8867 mL 7.2167 mL
15 mM 0.1924 mL 0.9622 mL 1.9244 mL 4.8111 mL
20 mM 0.1443 mL 0.7217 mL 1.4433 mL 3.6083 mL
25 mM 0.1155 mL 0.5773 mL 1.1547 mL 2.8867 mL
30 mM 0.0962 mL 0.4811 mL 0.9622 mL 2.4056 mL
40 mM 0.0722 mL 0.3608 mL 0.7217 mL 1.8042 mL
50 mM 0.0577 mL 0.2887 mL 0.5773 mL 1.4433 mL
60 mM 0.0481 mL 0.2406 mL 0.4811 mL 1.2028 mL
80 mM 0.0361 mL 0.1804 mL 0.3608 mL 0.9021 mL
100 mM 0.0289 mL 0.1443 mL 0.2887 mL 0.7217 mL
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Brevilin A 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.

Keywords:

Brevilin A16503-32-5JAKSTATApoptosisAutophagyJanus kinaseanti-tumor activityanti-proliferative activityinduce apoptosisinduce autophagyA549RCNE-2DU145MDA-MB-468Inhibitorinhibitorinhibit

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