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

Valecobulin hydrochloride  (Synonyms: CKD-516 hydrochloride)

Cat. No.: HY-13598A Purity: 98.58%
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Valecobulin hydrochloride (CKD-516 hydrochloride) is a valine proagent of S516 (HY-130233) and a vascular disrupting agent (VDA). Valecobulin hydrochloride is a potent β-tubulin polymerization inhibitor with marked antitumor activity against murine and human solid tumors.

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

Valecobulin hydrochloride Chemical Structure

Valecobulin hydrochloride Chemical Structure

CAS No. : 1240321-53-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 441 In-stock
Solution
10 mM * 1 mL in DMSO USD 441 In-stock
Solid
5 mg USD 350 In-stock
10 mg USD 550 In-stock
50 mg USD 1650 In-stock
100 mg USD 2250 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

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Based on 1 publication(s) in Google Scholar

Other Forms of Valecobulin hydrochloride:

Valecobulin hydrochloride Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

Valecobulin hydrochloride (CKD-516 hydrochloride) is a valine proagent of S516 (HY-130233) and a vascular disrupting agent (VDA). Valecobulin hydrochloride is a potent β-tubulin polymerization inhibitor with marked antitumor activity against murine and human solid tumors[1][2].

IC50 & Target

β-tubulin polymerization[1]
In Vivo

Valecobulin (5 mg/kg; intraperitoneal injection; administered on days 2, 6, 10, and 14; male BALB/C nu/nu mice) treatment shows markedly antitumor efficacy in various human tumor xenograft models[1].

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

Animal Model: Male BALB/C nu/nu mice (5-6 weeks of age) with HCT-116 or HCT-15 cells[1]
Dosage: 5 mg/kg
Administration: Intraperitoneal injection; administered on days 2, 6, 10, and 14
Result: Had shown marked antitumor efficacy in various human tumor xenograft models.
Clinical Trial
Molecular Weight

573.06

Formula

C26H29ClN6O5S
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

CC(C)[C@H](N)C(NC1=NC(C2=CC=C(C(C3=CC(OC)=C(OC)C(OC)=C3)=O)C(N4N=CN=C4)=C2)=CS1)=O.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (218.13 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 50 mg/mL (87.25 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7450 mL 8.7251 mL 17.4502 mL
5 mM 0.3490 mL 1.7450 mL 3.4900 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • 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: ≥ 2.25 mg/mL (3.93 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 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    90% Corn Oil

    Solubility: ≥ 2.25 mg/mL (3.93 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  PBS

    Solubility: 50 mg/mL (87.25 mM); Clear solution; Need ultrasonic

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.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
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 (sealed storage, away from moisture). 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
H2O / DMSO 1 mM 1.7450 mL 8.7251 mL 17.4502 mL 43.6254 mL
5 mM 0.3490 mL 1.7450 mL 3.4900 mL 8.7251 mL
10 mM 0.1745 mL 0.8725 mL 1.7450 mL 4.3625 mL
15 mM 0.1163 mL 0.5817 mL 1.1633 mL 2.9084 mL
20 mM 0.0873 mL 0.4363 mL 0.8725 mL 2.1813 mL
25 mM 0.0698 mL 0.3490 mL 0.6980 mL 1.7450 mL
30 mM 0.0582 mL 0.2908 mL 0.5817 mL 1.4542 mL
40 mM 0.0436 mL 0.2181 mL 0.4363 mL 1.0906 mL
50 mM 0.0349 mL 0.1745 mL 0.3490 mL 0.8725 mL
60 mM 0.0291 mL 0.1454 mL 0.2908 mL 0.7271 mL
80 mM 0.0218 mL 0.1091 mL 0.2181 mL 0.5453 mL
DMSO 100 mM 0.0175 mL 0.0873 mL 0.1745 mL 0.4363 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Valecobulin hydrochloride 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:

Valecobulin1240321-53-2CKD-516CKD516CKD 516Microtubule/TubulinS516VDAβ-tubulinantitumorprodrugInhibitorinhibitorinhibit

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