Physicochemical Properties
| Molecular Formula | C45H41N7O9 |
| Molecular Weight | 823.85 |
| Appearance | Solid powder |
| HS Tariff Code | 2934.99.9001 |
| Storage |
Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition | Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs) |
Biological Activity
| Targets | Cereblon NSD2 20 nM (DC50) |
| ln Vitro | LLC0424 dose-dependently inhibited the growth of SEM and RPMI-8402 cells with IC50 values of 3.56 μM and 0.56 μM, respectively[1]. LLC0424 (0.001 μM-10 μM; 1 hour-24 hours) induced NSD2 degradation in a concentration- and time-dependent manner, and in a CRBN- and proteasome-dependent manner. LLC0424 also led to downregulation of H3K36Me2[1]. |
| ln Vivo | LLC0424 (60 mg/kg; intravenous or intraperitoneal injection; 5 consecutive days) showed potent NSD2 degradation in vivo [1]. |
| Cell Assay |
Cell Viability Assay[1] Cell Types: SEM or RPMI-8402 Tested Concentrations: 5 μM Incubation Duration: 9 days (every 4 days) Experimental Results: Significantly inhibited the growth of SEM and RPMI-8402 cells. Western Blot Analysis[1] Cell Types: RPMI-8402 Tested Concentrations: 0.001 μM, 0.01 μM, 0.1 μM, 1 μM, and 10 μM Incubation Duration: 1 h, 2 h, 4 h, 6 h, 8 h, 12 h, 24 h Experimental Results: Reduced the protein level of both NSD2 isoforms in a concentration- and time-dependent manner. |
| Animal Protocol |
Animal/Disease Models:6-8 weeks old male CB17 severe combined immunodeficiency (SCID) mice injected with 22RV1 cells were injected[1] Doses: 60 mg/kg Route of Administration: Intravenous injection or intraperitoneal injection; for five consecutive days Experimental Results: Significantly downregulated the protein levels of NSD2. |
| References |
[1]. Discovery of LLC0424 as a Potent and Selective in Vivo NSD2 PROTAC Degrader. J Med Chem. 2024 May 9;67(9):6938-6951. |
Solubility Data
| Solubility (In Vitro) | DMSO : ≥ 100 mg/mL (121.38 mM) |
| 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 (e.g. IP/IV/IM/SC) Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline) *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). 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)] *Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline) Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline) Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline) Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil) Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL 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). Oral Formulation 3: Dissolved in PEG400 Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose Oral Formulation 6: Mixing with food powders Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.2138 mL | 6.0691 mL | 12.1381 mL | |
| 5 mM | 0.2428 mL | 1.2138 mL | 2.4276 mL | |
| 10 mM | 0.1214 mL | 0.6069 mL | 1.2138 mL |