LD-110 triTFA
Based on 1 Customer Validation
LD-110 triTFA is a PROTAC degrader targeting LSD1 with a DC50 of 0.44-1.24 μM. LD-110 triTFA acts through the CRBN E3 ubiquitin ligase and the ubiquitin-proteasome system, leading to H3K4me2 accumulation. LD-110 triTFA induces apoptosis and inhibits the growth and survival of multiple esophageal squamous cell carcinoma (ESCC) cell lines. LD-110 triTFA inhibits tumor growth in the KYSE-150 xenograft model. LD-110 triTFA can be used in research related to esophageal squamous cell carcinoma.
(Pink: LSD1 ligand (HY-178826); Blue: Cereblon ligand (HY-14658); Black: linker).
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity : 99.77%
- 화학식: C48H44F9N7O12
- 분자량:1081.89
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
All PROTACs Isoforms
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Biological Activity
제품 설명
IC50 & Target
[1]|
LSD1 0.44 μM (DC50, in KYSE-150 cells) |
LSD1 1.18 μM (DC50, in KYSE-30 cells) |
LSD1 1.24 μM (DC50, in EC9706 cells) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| KYSE-150 cell line | IC50 |
3.94 μM
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Inhibition of cell growth in human KYSE-150 esophagus squamous cancer cells incubated for 72 hrs by CCK-8 assay.
Inhibition of cell growth in human KYSE-150 esophagus squamous cancer cells incubated for 72 hrs by CCK-8 assay.
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41051788 |
| KYSE-30 | IC50 |
3.35 μM
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Inhibition of cell growth in human KYSE-30 esophagus squamous cancer cells incubated for 72 hrs by CCK-8 assay.
Inhibition of cell growth in human KYSE-30 esophagus squamous cancer cells incubated for 72 hrs by CCK-8 assay.
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41051788 |
| EC9706 | IC50 |
3.08 μM
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Inhibition of cell growth in human EC9706 esophagus squamous cancer cells incubated for 72 hrs by CCK-8 assay.
Inhibition of cell growth in human EC9706 esophagus squamous cancer cells incubated for 72 hrs by CCK-8 assay.
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41051788 |
In Vitro
LD-110 (10 μM; 6-72 h) triTFA degrades LSD1 and increases H3K4me2 levels in KYSE-150, KYSE-30, and EC9706 ESCC cells in a time-dependent manner[1].
LD-110 (48 h) triTFA treatment significantly increases H3K4me2 levels in KYSE-150, KYSE-30, and EC9706 ESCC cells[1].
LD-110 (0.1-30 μM; 48 h) triTFA potently and dose-dependently degrades LSD1 and induces H3K4me2 accumulation in KYSE-150, KYSE-30, and EC9706 esophageal squamous cell carcinoma cells[1].
LD-110 triTFA specifically degrades LSD1 in KYSE-150 cells without affecting the levels of other components of the LSD1 complex[1].
LD-110 (72 h) triTFA effectively inhibits the growth of KYSE-150, KYSE-30, and EC9706 ESCC cells with low micromolar IC50 values[1].
LD-110 (1-10 μM; 10-14 days) triTFA effectively inhibits clonogenic survival of KYSE-30 and EC9706 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:KYSE-150, KYSE-30, EC9706
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Concentration:10 μM
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Incubation Time:6, 12, 24, 48 and 72 h
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Result:Effectively reduced LSD1 protein levels after 24-48 h of treatment and achieved near-complete depletion of LSD1 at 48-72 h.
Caused the accumulation of H3K4me2.
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Cell Line:KYSE-150, KYSE-30, EC9706
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Concentration:0.1, 0.3, 1, 3, 10, 30 μM
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Incubation Time:48 h
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Result:Caused dose-dependent degradation of LSD1 with DC50 values of 0.44 μM in KYSE-150, 1.18 μM in KYSE-30, and 1.24 μM in EC9706 cells.
Caused dose-dependent accumulation of H3K4me2.
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Cell Line:KYSE-30, EC9706
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Concentration:1, 3 μM (KYSE-30); 3, 10 μM (EC9706)
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Incubation Time:10-14 days
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Result:Effectively suppressed the colony formation of ESCC cells in a dose-dependent manner.
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Cell Line:KYSE-30, EC9706
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Concentration:3, 10 μM
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Incubation Time:48 h
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Result:Induced both early-stage and late-stage apoptosis in a dose-dependent manner.
Induced dose-dependent cleavage of both PARP and caspase-3.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (male, age- and weight-matched)[1]
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Dosage:30 and 100 mg/kg
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Administration:i.p.; once daily; 24 days
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Result:Dose-dependently inhibited tumor growth at 30 and 100 mg/kg without affecting body weight.
Reduced LSD1 protein levels in tumor tissues at 100 mg/kg without causing morphological changes in major organs.
Suppressed in vivo tumor growth at 100 mg/kg without toxic effects on body weight, whereas LI-1 was largely ineffective at the same dose regimen.
Achieved tumor concentrations of 437 ng/g at 30 mg/kg and 946 ng/g at 100 mg/kg.
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Annexin V plus membrane-impermeant dye apoptosis staining
- Patient-Derived Xenograft (PDX)
- Apoptosis Solutions
- Patient-Derived Orthotopic Xenograft (PDOX)
- Splenic/Portal-Vein Liver Metastasis Xenograft
- Subcutaneous Cell-Line-Derived Xenograft
- Orthotopic Cell-Line Xenograft
- Intraperitoneal/Peritoneal Dissemination Xenograft
Chemical Information
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Appearance Solid
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분자량 1081.89
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화학식 C48H44F9N7O12
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Color Light yellow to yellow
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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
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
In Vitro:
DMSO : 100 mg/mL (92.43 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (2.31 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (2.31 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:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
순도&문서
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Data Sheet (283 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
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, 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 | 0.9243 mL | 4.6215 mL | 9.2431 mL | 23.1077 mL |
| 5 mM | 0.1849 mL | 0.9243 mL | 1.8486 mL | 4.6215 mL | |
| 10 mM | 0.0924 mL | 0.4622 mL | 0.9243 mL | 2.3108 mL | |
| 15 mM | 0.0616 mL | 0.3081 mL | 0.6162 mL | 1.5405 mL | |
| 20 mM | 0.0462 mL | 0.2311 mL | 0.4622 mL | 1.1554 mL | |
| 25 mM | 0.0370 mL | 0.1849 mL | 0.3697 mL | 0.9243 mL | |
| 30 mM | 0.0308 mL | 0.1541 mL | 0.3081 mL | 0.7703 mL | |
| 40 mM | 0.0231 mL | 0.1155 mL | 0.2311 mL | 0.5777 mL | |
| 50 mM | 0.0185 mL | 0.0924 mL | 0.1849 mL | 0.4622 mL | |
| 60 mM | 0.0154 mL | 0.0770 mL | 0.1541 mL | 0.3851 mL | |
| 80 mM | 0.0116 mL | 0.0578 mL | 0.1155 mL | 0.2888 mL |
LD-110 triTFA Related Classifications
HY-178825A Related Classifications
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