1. Immunology/Inflammation
  2. Galectin
  3. GB1908

GB1908 is a selective and orally active galectin-1 inhibitor with Ki values of 57 nM and 72 nM for human and mouse galectin-1, respectively. GB1908 displays >50-fold selectivity over galectin-3. GB1908 can be used for the study of lung cancer.

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GB1908

GB1908 Chemische Struktur

CAS. Nr. : 2573135-31-4

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Beschreibung

GB1908 is a selective and orally active galectin-1 inhibitor with Ki values of 57 nM and 72 nM for human and mouse galectin-1, respectively. GB1908 displays >50-fold selectivity over galectin-3. GB1908 can be used for the study of lung cancer[1].

IC50 & Target[1]

Galectin-1

57 nM (Ki, Human galectin-1)

Galectin-1

72 nM (Ki, Mouse galectin-1)

Galectin-3

6000 nM (Ki, Human galectin-3)

Galectin-3

4200 nM (Ki, Mouse galectin-3)

Cellular Effect
Cell Line Type Value Description References
Jurkat IC50
0.85 3
Compound: 5d
Inhibition of apoptosis in galectin-1-induced human Jurkat cells measured after 16 hrs by caspase-3/7 green fluorescence based analysis
Inhibition of apoptosis in galectin-1-induced human Jurkat cells measured after 16 hrs by caspase-3/7 green fluorescence based analysis
[PMID: 38804039]
Jurkat IC50
> 8 3
Compound: 5d
Inhibition of apoptosis in galectin-3-induced human Jurkat cells measured after 16 hrs by caspase-3/7 green fluorescence based analysis
Inhibition of apoptosis in galectin-3-induced human Jurkat cells measured after 16 hrs by caspase-3/7 green fluorescence based analysis
[PMID: 38804039]
In Vitro

GB1908 (0.1-10 μM; 16 h) inhibits galectin-1-induced apoptosis in Jurkat cells (IC50 of 850 nM)[1].

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

Apoptosis Analysis[1]

Cell Line: Jurkat cells treatment with galectin-1
Concentration: 0.1-10 μM
Incubation Time: 16 h
Result: Inhibited galectin-1-induced apoptosis.
In Vivo

GB1908 (compound 5d; 30 mg/kg; po; twice a day; for 21 days) reduces the growth of primary lung tumor LL/2 in a syngeneic mouse model[1].

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

Animal Model: Female C57BL/6N mice injected with LL/2 (LLC1) Lewis lung carcinoma cells[1]
Dosage: 30 mg/kg (PEG300/Solutol HS15/Tween 20 solution (85/15/1% v/v))
Administration: po; twice a day; for 21 days
Result: Significantly inhibited tumor growth.
Molekulargewicht

505.40

Formel

C18H18Cl2N4O5S2

CAS. Nr.
Appearance

Solid

Color

Off-white to light yellow

SMILES

ClC1=CC(S[C@H]2O[C@H](CO)[C@H](O)[C@H](N3C=C(C4=CSC(O)=N4)N=N3)[C@H]2OC)=CC=C1Cl

Versand

Room temperature in continental US; may vary elsewhere.

Speicherung
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Lösungsmittel & Löslichkeit
In Vitro: 

DMSO : 100 mg/mL (197.86 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 1.9786 mL 9.8932 mL 19.7863 mL
5 mM 0.3957 mL 1.9786 mL 3.9573 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.

  • Molaritätsrechner

  • Verdünnungsrechner

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 (4.95 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.
  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (4.95 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.
Reinheit & Dokumentation
Verweise

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 1.9786 mL 9.8932 mL 19.7863 mL 49.4658 mL
5 mM 0.3957 mL 1.9786 mL 3.9573 mL 9.8932 mL
10 mM 0.1979 mL 0.9893 mL 1.9786 mL 4.9466 mL
15 mM 0.1319 mL 0.6595 mL 1.3191 mL 3.2977 mL
20 mM 0.0989 mL 0.4947 mL 0.9893 mL 2.4733 mL
25 mM 0.0791 mL 0.3957 mL 0.7915 mL 1.9786 mL
30 mM 0.0660 mL 0.3298 mL 0.6595 mL 1.6489 mL
40 mM 0.0495 mL 0.2473 mL 0.4947 mL 1.2366 mL
50 mM 0.0396 mL 0.1979 mL 0.3957 mL 0.9893 mL
60 mM 0.0330 mL 0.1649 mL 0.3298 mL 0.8244 mL
80 mM 0.0247 mL 0.1237 mL 0.2473 mL 0.6183 mL
100 mM 0.0198 mL 0.0989 mL 0.1979 mL 0.4947 mL
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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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