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).
For research use only. We do not sell to patients.
- Purity : 99.77%
- Formula: C48H44F9N7O12
- Molecular Weight:1081.89
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Storage: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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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
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 |
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| 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 (1-10 μM) triTFA effectively degrades LSD1 protein in a dose-dependent manner in KYSE-150 cells[1].
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].
LD-110 (3-10 μM; 48 h) triTFA induces apoptosis in KYSE-30 and EC9706 esophageal squamous cell carcinoma cells in a dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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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.
Chemical Information
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Appearance Solid
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Molecular Weight 1081.89
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
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.
Protocols
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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Patient-Derived Xenograft (PDX)
Patient-derived xenograft (PDX) models are generated by engrafting primary human tumor tissue directly into immunodeficient mice, allowing in vivo propagation of patient tumor biology without initial in vitro adaptation. These models are used to preserve key histopathological and molecular characteristics of the original tumor and enable assessment of tumor growth dynamics and therapeutic response in a living organism. The biological readout is tumor engraftment and subsequent growth in the murine host, which reflects the ability of human tumor cells to survive, vascularize, and expand in an immunocompromised microenvironment.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
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Patient-Derived Orthotopic Xenograft (PDOX)
Patient-derived orthotopic xenograft (PDOX) modeling implants fresh patient tumor tissue or patient-derived tumor cells into the anatomically corresponding organ or tissue site of immunodeficient mice, usually by surgical orthotopic implantation, to preserve patient tumor histology, local microenvironmental context, invasion, metastatic behavior, and treatment-response features better than subcutaneous implantation. PDOX readouts include tumor engraftment, orthotopic tumor growth, local invasion, metastasis, recurrence after resection, histologic similarity to the donor tumor, biomarker retention, molecular concordance, survival, and response or resistance to therapy. PDOX models are used for preclinical drug testing and individualized therapy evaluation, but engraftment success varies by tumor type and specimen quality.
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Splenic/Portal-Vein Liver Metastasis Xenograft
Splenic and portal-vein liver metastasis xenograft models deliver tumor cells into the portal circulation so that cells reach the liver first and form hepatic metastatic lesions; splenic injection uses the spleen as an access route to the portal system, while direct portal-vein injection introduces cells into the portal vein without requiring splenectomy. The assay detects liver colonization, intrahepatic tumor growth, tumor distribution, treatment response, survival, and liver-metastasis microenvironment changes; readouts include bioluminescence or fluorescence imaging, gross liver nodule counts, liver weight or tumor burden, histology, and survival.
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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
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Orthotopic Cell-Line Xenograft
Orthotopic cell-line xenograft models involve implantation of human cancer cell lines into the anatomically corresponding organ of immunodeficient mice to reproduce tumor growth within a native microenvironment, enabling more clinically relevant tumor behavior compared with subcutaneous models. These models are widely used because orthotopic placement better recapitulates tumor progression, including invasion and metastatic spread, which are often underrepresented in heterotopic implantation systems. Compared with conventional xenografts, orthotopic implantation is described as more technically complex but provides improved simulation of tumor-microenvironment interactions and metastatic behavior, making it particularly valuable for translational oncology research. Surgical orthotopic implantation approaches have been emphasized as enabling faithful reproduction of clinical cancer features, including metastasis and disease progression patterns that align with the tumor’s organ of origi
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Intraperitoneal/Peritoneal Dissemination Xenograft
Intraperitoneal (IP) or peritoneal dissemination xenograft models are based on the introduction of human cancer cells into the peritoneal cavity of immunodeficient mice, where they attach to peritoneal surfaces, form multicellular aggregates or spheroids, and progressively generate disseminated tumor nodules that mimic advanced peritoneal metastatic disease. These models are widely used to study ovarian cancer progression, tumor-microenvironment interactions, and intraperitoneal therapeutic responses, often incorporating bioluminescence or fluorescence imaging to longitudinally monitor tumor burden in vivo. The biological principle relies on the capacity of tumor cells such as SKOV3 or related ovarian carcinoma lines to survive in suspension, aggregate within ascites-like fluid, adhere to mesothelial surfaces, and invade peritoneal organs, thereby recapitulating human peritoneal carcinomatosis patterns observed in advanced disease.
Purity & Documentation
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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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