1. Metabolic Enzyme/Protease
  2. Sialyltransferase
  3. Lith-O-Asp

Lith-O-Asp is a sialytransferase (ST) inhibitor, with IC50s of 12-37 μM.

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

Lith-O-Asp Chemical Structure

Lith-O-Asp Chemical Structure

CAS No. : 881179-02-8

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 605 In-stock
Solution
10 mM * 1 mL in DMSO USD 605 In-stock
Solid
5 mg USD 550 In-stock
10 mg USD 850 In-stock
25 mg USD 1750 In-stock
50 mg USD 2750 In-stock
100 mg USD 3950 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Lith-O-Asp

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Lith-O-Asp is a sialytransferase (ST) inhibitor, with IC50s of 12-37 μM.

IC50 & Target

IC50: 12-37 μM (ST)[1].

In Vitro

The results indicate that Lith-O-Asp shows no apparent growth inhibition effect toward different cancer cell lines at the tested doses of 10, 30, and 60 μM. By in vitro activity assay, it is revealed that the ability of Lith-O-Asp to inhibit the activities of ST3Gal I, ST3Gal III, and ST6GalI. The IC50 values ranged from 12 to 37 μM. Flow cytometry shows a significant decrease in the expression of cell surface a-2,3- and a-2,6-sialylated antigens on The results indicates that Lith-O-Asp decreased the activity of both a-2,3- and a-2,6-sialyltransferases, and thus inhibit the transfer of sialic acids to the targeted glycoproteins[1].

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

In Vivo

A significant amount of secondary metastatic cancer cells are observed in lung tissues of DMSO control mice detected using IVIS in vivo imaging system after 26 days of fat pad inoculation. However, Lith-O-Asp–treated mice show fewer lung metastases. All DMSO-treated mice confirm secondary lung metastasis, but only 3 of 8 Lith-O-Asp-treated mice show lung metastasis. Average tumor nodules per mouse are 11±9 nodules in DMSO-treated group, and 2±4 nodules in Lith-O-Asp-treated group. Additionally, significantly stronger 4T1-Luc illumination signals are shown in control mice than in those injected with Lith-O-Asp-treated cancer cells on days 7 and 9[1].

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

Molecular Weight

491.66

Formula

C28H45NO6

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C[C@@]12[C@](CC[C@]2([H])[C@H](C)CCC(O)=O)([H])[C@@]3([H])[C@]([C@@]4([C@](C[C@H](OC([C@@H](N)CC(O)=O)=O)CC4)([H])CC3)C)([H])CC1

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 (203.39 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 2.0339 mL 10.1696 mL 20.3393 mL
5 mM 0.4068 mL 2.0339 mL 4.0679 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    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.5 mg/mL (5.08 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.08 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 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
References
Cell Assay
[1]

About 3x104 of the CL1-0, CL1-5, A549, and H1299 lung cancer cells are seeded on 12-well culture dishes in DMEM containing 10% FBS. Different concentrations of Lith-O-Asp (10, 30, and 60 μM) are added into each plate and incubated for 48 hr. Cell viabilities under different concentrations of compound treatment are determined by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay. In the untreated control, 0.1% DMSO-containing medium is used[1].

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

Animal Administration
[1]

Mice[1]
The BALB/c mice are used. Highly metastatic murine 4T1-Luc breast cancer cells (5 x105) are subcutaneously injected into the mammary fat pad of mice. Mice receive 3 mg/kg of Lith-O-Asp intraperitoneally on every other day. DMSO treatment is used as control. The growth and the spontaneous metastasis of the tumors are observed under IVIS50 in vivo imaging system with endotoxin-free luciferase substrate injection. The metastasized tumor tissues are dissected on day 26[1].

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

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 2.0339 mL 10.1696 mL 20.3393 mL 50.8481 mL
5 mM 0.4068 mL 2.0339 mL 4.0679 mL 10.1696 mL
10 mM 0.2034 mL 1.0170 mL 2.0339 mL 5.0848 mL
15 mM 0.1356 mL 0.6780 mL 1.3560 mL 3.3899 mL
20 mM 0.1017 mL 0.5085 mL 1.0170 mL 2.5424 mL
25 mM 0.0814 mL 0.4068 mL 0.8136 mL 2.0339 mL
30 mM 0.0678 mL 0.3390 mL 0.6780 mL 1.6949 mL
40 mM 0.0508 mL 0.2542 mL 0.5085 mL 1.2712 mL
50 mM 0.0407 mL 0.2034 mL 0.4068 mL 1.0170 mL
60 mM 0.0339 mL 0.1695 mL 0.3390 mL 0.8475 mL
80 mM 0.0254 mL 0.1271 mL 0.2542 mL 0.6356 mL
100 mM 0.0203 mL 0.1017 mL 0.2034 mL 0.5085 mL
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Lith-O-Asp 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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Lith-O-Asp
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