| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
LD-110 (1-10 μM) triTFA, whose linker contains four methylene groups, exhibits good degradation activity. At concentrations of 1, 3 and 10 μM, the degradation rates of LSD1 protein are 65%, 70% and 84%, respectively [1]. LD-110 (0.1-30 μM, 6-72 h) triTFA can effectively and dose-dependently degrade LSD1 protein, achieving near-complete degradation within 48-72 hours. The DC50 values in KYSE-150, KYSE-30 and EC9706 esophageal squamous cell carcinoma (ESCC) cells are 0.44, 1.18 and 1.24 μM, respectively. This degradation is highly specific and has minimal effect on CoREST/HDAC1/HDAC2 levels, thus leading to a significant accumulation of H3K4me2 by 2 to 7 times [1]. LD-110 (72 h) triTFA effectively inhibited the growth of esophageal squamous cell carcinoma (ESCC) cells, with half-maximal inhibitory concentrations (IC50) of 3.94, 3.35, and 3.08 μM in KYSE-150, KYSE-30, and EC9706 cells, respectively [1]. LD-110 (3-10 μM, 10-14 days) triTFA effectively inhibited the proliferation of ESCC KYSE-30 and EC9706 cells [1]. LD-110 (3-10 μM, 48 h) triTFA induced early and late apoptosis in KYSE-30 and EC9706 cells in a dose-dependent manner and led to the lysis of PARP and caspase-3 [1].
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|---|---|
| ln Vivo |
LD-110 (30 mg/kg, 100 mg/kg, intraperitoneal injection, once daily for 24 days) triTFA showed strong dose-dependent antitumor activity in the KYSE-150 xenograft mouse model without causing significant toxicity [1].
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| Cell Assay |
Western Blot Analysis [1]
Cell Types: KYSE-150, KYSE-30 and EC9706 esophageal squamous cell carcinoma (ESCC) cells Tested Concentrations: 10 μM Incubation Duration: 6 h, 12 h, 24 h, 48 h, 72 h Experimental Results: After treatment for 24-48 hours, LSD1 protein levels decreased significantly, and after 48-72 hours, LSD1 was almost completely depleted, leading to the accumulation of H3K4me2. Western Blot Analysis [1] Cell Types: KYSE-150, KYSE-30, and EC9706 esophageal squamous cell carcinoma (ESCC) cells Tested Concentrations: 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, 30 μM Incubation Duration: 48 hours Experimental Results: In KYSE-150, KYSE-30, and EC9706 cells, LSD1 degradation was dose-dependent, with DC50 values of 0.44, 1.18, and 1.24 μM, respectively. H3K4me2 accumulation was also dose-dependent. |
| Animal Protocol |
Animal/Disease Models:KYSE-150 cells were injected bilaterally into male BALB/c nude mice [1].
Doses: 30 mg/kg, 100 mg/kg Route of Administration: Intraperitoneal injection, once daily for 24 days Experimental Results: Intraperitoneal injection of 30 mg/kg and 100 mg/kg doses dose-dependently inhibited tumor growth without affecting body weight. The 100 mg/kg dose also effectively reduced the level of LSD1 protein in tumor tissues collected at the end of the study without causing any morphological changes in major organs, including the heart, liver, spleen, lungs, and kidneys. |
| References |
| Molecular Formula |
C48H44F9N7O12
|
|---|---|
| Molecular Weight |
1081.89
|
| Appearance |
Light yellow to yellow solid
|
| SMILES |
O=C(NCCCCNC1=CC2=C(C(N(C(CC3)C(NC3=O)=O)C2=O)=O)C=C1)C4=CC=C(C5=NC=C(OCC6CCNCC6)C=C5C7=CC=C(C#N)C=C7)C=C4.OC(C(F)(F)F)=O.OC(C(F)(F)F)=O.OC(C(F)(F)F)=O
|
| 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 |
| 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 : ~100 mg/mL (~92.43 mM; with sonication)
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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 | 0.9243 mL | 4.6215 mL | 9.2431 mL | |
| 5 mM | 0.1849 mL | 0.9243 mL | 1.8486 mL | |
| 10 mM | 0.0924 mL | 0.4622 mL | 0.9243 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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