2. Protein Tyrosine Kinase/RTK Apoptosis
  3. Anaplastic lymphoma kinase (ALK) Apoptosis
  4. W23-1006

W23-1006 is a selective and covalent ALKBH5 inhibitor. W23-1006 binds to the ALKBH5 C200 residue with an IC50 value of 3.848 μM. W23-1006 shows ~30- and 8-fold stronger inhibitory activity than that against FTO and ALKBH3, respectively. W23-1006 can be used for the study of triple-negative breast cancer (TNBC).

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W23-1006

W23-1006 Chemical Structure

CAS No. : 3035498-92-8

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
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Based on 1 publication(s) in Google Scholar

W23-1006 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

W23-1006 is a selective and covalent ALKBH5 inhibitor. W23-1006 binds to the ALKBH5 C200 residue with an IC50 value of 3.848 μM. W23-1006 shows ~30- and 8-fold stronger inhibitory activity than that against FTO and ALKBH3, respectively. W23-1006 can be used for the study of triple-negative breast cancer (TNBC)[1].

In Vitro

W23-1006 (5 μM; 24 h) significantly increases the mA abundance in MDA-MB-231 and BT549 cells[1].
W23-1006 (3.16-31.6 μM; 24 h) inhibits the cell viability of MDA-MB-231 and BT549[1].
W23-1006 (5 μM) could obviously reduce TNBC cell colonization area and suppress cell migration[1].
W23-1006 (5-10 μM) induces the apoptosis and decreases the G2/M phase of MDA-MB-231 cells[1].

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

W23-1006 Related Antibodies

RT-PCR[1]

Cell Line: MDA-MB-231 and BT549 cells
Concentration: 5 μM
Incubation Time: 24 h
Result: The mA abundance significantly increased in cells.

Cell Viability Assay[1]

Cell Line: MDA-MB-231 and BT549 cells
Concentration: 3.16 μM, 10 μM, 31.62 μM
Incubation Time: 24 h
Result: Inhibited cell viability of MDA-MB-231 and BT549 with IC50 values of 10.31 μM and 6.338 μM, respectively.
In Vivo

W23-1006 (25 mg/kg; intraperitoneal injection (i.p.); once daily; for 14 days) exerts antitumor efects on breast cancer in vivo[1].
W23-1006 (25 mg/kg; i.p.; once daily; for 10 days) could obviously inhibit TNBC lung metastasis[1].
W23-1006 (single dosage at 25 mg/kg; i.p.) shows the t1/2 ranged from 0.509 to 0.983 h, and the Cmax in plasma (in the range of 1715-2108 ng/mL) is reached 15 min in mice[1].
Neither 100 mg/kg nor 250 mg/kg dosage of W23-1006 (i.p.) causes adverse events or death in KM mice (22-27g)[1].

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

Animal Model: Immunodefcient female mouse was subcutaneously injected MDA-MB-231 cells[1].
Dosage: 25 mg/kg (5% DMSO, 10% Kolliphor HS 15, and 85% saline)
Administration: Intraperitoneal injection; once daily; for 14 days
Result: Apparently reduced the tumor volume and weight.
Strongly reduced the FN1 and Ki-67 protein expression level.
Animal Model: Immunodefcient female mouse injected MDA-MB-231LMF3 through the tail vein[1].
Dosage: 25 mg/kg
Administration: Intraperitoneal injection; once daily; for 10 days
Result: Inhibited TNBC lung metastasis.
No apparent pathologic abnormality was observed in the HEstaining results of multiple organs, including heart, liver,spleen, lung, and kidney.
There was no signifcant diference in glutamic pyruvic transaminase(ALT) and glutamic oxaloacetic transaminase (AST) levels in mouse serum, did not infuence mice liver function.
Molecular Weight

418.20

Formula

C17H12BrN3O5
CAS No.
Appearance

Solid

Color

Brown to reddish brown

SMILES

O=C(/C1=C\C2=CC([N+]([O-])=O)=CC(Br)=C2)NN(C3=CC=C(C=C3)OC)C1=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (239.12 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 2.3912 mL 11.9560 mL 23.9120 mL
5 mM 0.4782 mL 2.3912 mL 4.7824 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 (stored under nitrogen). 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
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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

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Volume (start)

V1

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Concentration (final)

C2

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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: ≥ 2.5 mg/mL (5.98 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.
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).

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

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, 6 months; -20°C, 1 month (stored under nitrogen). 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 2.3912 mL 11.9560 mL 23.9120 mL 59.7800 mL
5 mM 0.4782 mL 2.3912 mL 4.7824 mL 11.9560 mL
10 mM 0.2391 mL 1.1956 mL 2.3912 mL 5.9780 mL
15 mM 0.1594 mL 0.7971 mL 1.5941 mL 3.9853 mL
20 mM 0.1196 mL 0.5978 mL 1.1956 mL 2.9890 mL
25 mM 0.0956 mL 0.4782 mL 0.9565 mL 2.3912 mL
30 mM 0.0797 mL 0.3985 mL 0.7971 mL 1.9927 mL
40 mM 0.0598 mL 0.2989 mL 0.5978 mL 1.4945 mL
50 mM 0.0478 mL 0.2391 mL 0.4782 mL 1.1956 mL
60 mM 0.0399 mL 0.1993 mL 0.3985 mL 0.9963 mL
80 mM 0.0299 mL 0.1495 mL 0.2989 mL 0.7473 mL
100 mM 0.0239 mL 0.1196 mL 0.2391 mL 0.5978 mL
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W23-1006 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:

W23-10063035498-92-8Anaplastic lymphoma kinase (ALK)ApoptosisAnaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246ALKBH5 inhibitortriple-negative breast cancer (TNBC)induces the apoptosisdecreases the G2/M phaseantitumor efectsInhibitorinhibitorinhibit

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