LD-110 triTFA |
Catalog No.GC80877
One-Click Copy Product Info
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LD-110 triTFA is a highly efficient and effective LSD1 PROTAC degrader ( DC50 = 0.44 μM).
Products are for research use only. Not for human use. We do not sell to patients.
Sample solution is provided at 25 µL, 10mM.
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In Vivo, LD-110 (30 mg/kg, 100 mg/kg, i.p., once daily for 24 days) triTFA exhibits potent dose-dependent antitumor activity in the KYSE-150 xenograft mice model without causing significant toxicity[1].
In Vitro, LD-110 (1-10 μM) triTFA, with a linker containing four methylene groups, demonstrates good degradation activity, achieving degradation rates of 65, 70, and 84% against the LSD1 protein at concentrations of 1, 3, and 10 μM, respectively[1]. LD-110 (0.1-30 μM, 6-72 h) triTFA effectively and dose-dependently degrades LSD1 protein, achieving near-complete depletion within 48-72 hours with DC50 values of 0.44, 1.18, and 1.24 μM in KYSE-150, KYSE-30, and EC9706 ESCC cells, respectively; this degradation is highly specific with minimal effect on CoREST/HDAC1/HDAC2 levels, and consequently leads to a potent 2 to 7-fold accumulation of H3K4me2[1]. LD-110 (72 h) triTFA effectively suppresses the growth of ESCC cells with half-maximal inhibitory concentration (IC50) values of 3.94, 3.35, and 3.08 μM in KYSE-150, KYSE-30, and EC9706, respectively[1]. LD-110 (3-10 μM, 10-14 days) triTFA can effectively inhibit the proliferation of ESCC KYSE-30 and EC9706 cells[1]. LD-110 (3-10 μM, 48 h) triTFA dose-dependently induces both early-stage and late-stage apoptosis and causes cleavage of PARP and caspase-3 in KYSE-30 and EC9706 cells[1].
References:
[1]. Zhuo J, et al. Discovery of LD-110 as an Effective LSD1 PROTAC Degrader for the Treatment of Esophagus Squamous Cancer. J Med Chem. 2025 Oct 23;68(20):21860-21877.
| Cas No. | SDF | ||
| Formula | C48H44F9N7O12 | M.Wt | 1081.89 |
| Solubility | DMSO: 100 mg/mL (92.43 mM; Need ultrasonic) | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 924.3 μL | 4.6215 mL | 9.2431 mL |
| 5 mM | 184.9 μL | 924.3 μL | 1.8486 mL |
| 10 mM | 92.4 μL | 462.2 μL | 924.3 μL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)