| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Targets |
G3BP2[1]
The primary target of Compound C108 is the GTPase-activating protein SH3 domain-binding protein 2 (G3BP2). G3BP2 is a stress granule-associated protein reported to bind and stabilize SART3 mRNA, thereby indirectly regulating the core pluripotency transcription factors Oct-4 and Nanog, which are critical for embryonic stem cell self-renewal and breast tumor initiation. |
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| ln Vitro |
On BT474 cells, compound C108 (1 μM; 24 h) exhibits anti-tumor activity [1]. Compound C108 (4 μM; 24 h) dramatically lowers the G3BP2 protein expression in KYSE410 cells that overexpress G3BP2 and KYSE30 cells that have been transfected with LINC01554. Compound C108 (4 μM; 24 h) inhibits KYSE410, KYSE30, and KYSE150 cell invasion, migration, and metastasis of ESCC cells [2].
In BT474 cells, Compound C108 (1 μM) shows anti-tumor activity. In G3BP2-overexpressing KYSE410 cells and LINC01554-transfected KYSE30 cells, Compound C108 (4 μM) reduces G3BP2 protein expression and attenuates ESCC cell metastasis, migration, and invasion. It exhibits cancer-selective cytotoxicity, with viability at 100% in MCF-10A cells vs. 50% in BT-474 cells post 48h 1 μM treatment. |
| ln Vivo |
When Compound C108-treated BT-474 cells are implanted into female non-obese diabetic/severe combined immunodeficient (NOD-SCID) mice, the compound targets and decreases tumor-initiating cells (TICs) (1 μM; 24 h). Tumor-initiating cells (TICs) in limited dilution xenograft experiments in the mammary fat pad were reduced as a result of compound C108 [1].
In a mouse xenograft model of breast cancer, Compound C108 (1 μM for 24 hours) reduces the proportion of tumor-initiating cells approximately 10-fold compared with untreated cells. Likewise, C108 pretreatment prior to xenografting greatly reduces BT-474 tumor-initiating frequency (from 1/175 to 1/1103 by limiting dilution xenograft assays) in mice in vivo. |
| Enzyme Assay |
Non-cellular assays for Compound C108 are not extensively detailed in the available literature. As a small-molecule inhibitor (MW 270.28), its activity is typically characterized through target engagement studies, such as surface plasmon resonance (SPR) or isothermal titration calorimetry (ITC), to determine binding affinity to the G3BP2 protein. Standard biochemical assays may be employed to confirm its mechanism of action.
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| Cell Assay |
Western Blot Analysis[2]
Cell Types: G3BP2-overexpressing KYSE410 cells, LINC01554-transfected KYSE30 cells Tested Concentrations: 4 μM Incubation Duration: 24 h Experimental Results: diminished the protein level of G3BP2 and HDGF. Cellular assays for Compound C108 are conducted using various cancer cell lines. In BT474 cells, the compound is used at 1 μM to assess anti-tumor activity. In G3BP2-overexpressing KYSE410 cells and LINC01554-transfected KYSE30 cells, Compound C108 (4 μM; 24 h) is used to evaluate G3BP2 protein expression via Western blot, and to assess ESCC cell metastasis, migration, and invasion. Cell viability is measured using standard assays like MTT. |
| Animal Protocol |
In vivo animal experiments for Compound C108 typically use a mouse xenograft model of breast cancer. In one protocol, BT-474 cells are pretreated with Compound C108 (1 μM for 24 hours) prior to xenografting into mice. The tumor-initiating frequency is then assessed by limiting dilution xenograft assays, demonstrating a reduction from 1/175 to 1/1103.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Compound C108 are not extensively detailed. The compound has a molecular weight of 270.28 and a molecular formula of C15H14N2O3. It is soluble in DMSO (11.36 mg/mL) and DMF. For in vivo studies, it can be formulated using a vehicle such as 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% saline.
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| Toxicity/Toxicokinetics |
Toxicological data for Compound C108 are limited. It exhibits cancer-selective cytotoxicity, with significantly lower toxicity to non-cancerous cells (e.g., MCF-10A) compared to cancer cell lines. The compound is classified with hazard warnings for Eye Irrit. 2 and Skin Irrit. 2. It is for research use only and not for human or veterinary use.
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| References |
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| Additional Infomation |
Compound C108 is a G3BP2 inhibitor used in research on breast tumors and esophageal squamous cell carcinoma. It synergizes with low-dose paclitaxel against tumor-initiating cell populations in breast cancer cultures. G3BP2 inhibition by Compound C108 has also been shown to suppress TNF-α-induced rheumatoid arthritis fibroblast-like synoviocyte migration and invasion, and it has been proposed for treating autism spectrum disorder by inhibiting stress granule formation.
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| Molecular Formula |
C15H14N2O3
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|---|---|
| Molecular Weight |
270.28
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| Exact Mass |
270.1
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| CAS # |
15533-09-2
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| PubChem CID |
135472588
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Index of Refraction |
1.607
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| LogP |
3.52
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
20
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| Complexity |
370
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C/C(=N\NC(=O)C1=CC=CC=C1O)/C2=CC=CC=C2O
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| InChi Key |
LQGMBUGEAAGJKW-MHWRWJLKSA-N
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| InChi Code |
InChI=1S/C15H14N2O3/c1-10(11-6-2-4-8-13(11)18)16-17-15(20)12-7-3-5-9-14(12)19/h2-9,18-19H,1H3,(H,17,20)/b16-10+
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| Chemical Name |
2-hydroxy-N-[(E)-1-(2-hydroxyphenyl)ethylideneamino]benzamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 25 mg/mL (92.50 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.6999 mL | 18.4993 mL | 36.9987 mL | |
| 5 mM | 0.7400 mL | 3.6999 mL | 7.3997 mL | |
| 10 mM | 0.3700 mL | 1.8499 mL | 3.6999 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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