2. Cell Cycle/DNA Damage Cytoskeleton
  3. Microtubule/Tubulin
  4. S516

S516 (Compound 22) is an active metabolite of CKD-516 and a potent tubulin polymerization inhibitor with an IC50 of 4.29 μM. S516 has marked antitumor activity.

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

S516 Chemical Structure

S516 Chemical Structure

CAS No. : 1016543-77-3

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 308 In-stock
Solution
10 mM * 1 mL in DMSO USD 308 In-stock
Solid
5 mg USD 280 In-stock
10 mg USD 450 In-stock
25 mg USD 850 In-stock
50 mg USD 1280 In-stock
100 mg USD 1950 In-stock
200 mg   Get quote  
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of S516:

S516 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

S516 (Compound 22) is an active metabolite of CKD-516 and a potent tubulin polymerization inhibitor with an IC50 of 4.29 μM. S516 has marked antitumor activity[1].

IC50 & Target

IC50: 4.29 μM (tubulin polymerization)[1]
Cellular Effect
Cell Line Type Value Description References
HCT-116 IC50
42.8 nM
Compound: 22
Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay
Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay
[PMID: 20690624]
HCT-15 IC50
24.9 nM
Compound: 22
Cytotoxicity against human HCT15 cells after 72 hrs by MTT assay
Cytotoxicity against human HCT15 cells after 72 hrs by MTT assay
[PMID: 20690624]
HCT-15 IC50
4.29 μM
Compound: 22
Inhibition of tubulin polymerization in multidrug-resistant human HCT15 cells after 1 hr
Inhibition of tubulin polymerization in multidrug-resistant human HCT15 cells after 1 hr
[PMID: 20690624]
HL-60 IC50
0.0048 μM
Compound: 1
Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay
Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay
[PMID: 20850313]
HL-60 IC50
4.8 nM
Compound: 22
Cytotoxicity against human HL60 cells after 72 hrs by MTT assay
Cytotoxicity against human HL60 cells after 72 hrs by MTT assay
[PMID: 20690624]
MDA-MB-231 IC50
9.8 nM
Compound: 1
Antiproliferative activity against P-gp expressing multidrug-resistant human MDA-MB-231 cells after 72 hrs by MTT assay
Antiproliferative activity against P-gp expressing multidrug-resistant human MDA-MB-231 cells after 72 hrs by MTT assay
[PMID: 20850313]
In Vitro

S516 has potent cytotoxicity with IC50s of 4.8 nM, 42.8 nM and 24.9 nM for HL-60, HCT116 and HCT15 cells, respectively[1].
S516 (Compound 22; 30 nM; 16 hours; HL60 cells) treatmemt causes significant arrest of cells at the G2/M phase, resulting in apoptosis with concomitant loss of G0/G1 phase[1].

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

S516 Related Antibodies

Cell Cycle Analysis[1]

Cell Line: HL60 cells
Concentration: 30 nM
Incubation Time: 16 hours
Result: Caused significant arrest of cells at the G2/M phase, resulting in apoptosis with concomitant loss of G0/G1 phase.
In Vivo

S516 (Compound 22; 5-10 mg/kg; intraperitoneal injection; mice) treatment has promising antitumor activity (inhibition ratio (IR)> 63%) in human LX-1 lung cancer and CX-1 colon cancer mouse xenografts[1].

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

Animal Model: Mice bearing 3LL lung cancer[1]
Dosage: 5 mg/kg, 10 mg/kg
Administration: Intraperitoneal injection
Result: Had promising antitumor activity (inhibition ratio (IR)> 63%).
Molecular Weight

437.47

Formula

C21H19N5O4S
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=CC=C(C2=CSC(N)=N2)C=C1N3N=CN=C3)C4=CC(OC)=C(OC)C(OC)=C4
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 : 12.5 mg/mL (28.57 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 2.2859 mL 11.4294 mL 22.8587 mL
5 mM 0.4572 mL 2.2859 mL 4.5717 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: ≥ 1.25 mg/mL (2.86 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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
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 2.2859 mL 11.4294 mL 22.8587 mL 57.1468 mL
5 mM 0.4572 mL 2.2859 mL 4.5717 mL 11.4294 mL
10 mM 0.2286 mL 1.1429 mL 2.2859 mL 5.7147 mL
15 mM 0.1524 mL 0.7620 mL 1.5239 mL 3.8098 mL
20 mM 0.1143 mL 0.5715 mL 1.1429 mL 2.8573 mL
25 mM 0.0914 mL 0.4572 mL 0.9143 mL 2.2859 mL
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S516 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:

S5161016543-77-3S 516S-516Microtubule/TubulinInhibitorinhibitorinhibit

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