TD-165

TD-165 is a PROTAC-based cereblon (CRBN) degrader. TD-165 comprises a cereblon (CRBN) ligand binding group, a linker and an von Hippel-Landau (VHL) binding group.

TD-165 Chemical Structure

TD-165 Chemical Structure

CAS: 2305936-56-3

Purity & Quality Control

Batch: S699401 DMSO] 100 mg/mL] false] Ethanol] 100 mg/mL] false] Water] Insoluble] false Purity: 99.92%
99.92

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Biological Activity

Description TD-165 is a PROTAC-based cereblon (CRBN) degrader. TD-165 comprises a cereblon (CRBN) ligand binding group, a linker and an von Hippel-Landau (VHL) binding group.
Targets
CRBN [1]
20.4 nM(DC50)
In vitro
In vitro

Treatment with TD-165 causes a concentration-dependent decrease in the level of CRBN proteins by Western blot analysis.[1]

Cell Research Cell lines HEK293T cells
Concentrations 0.1, 1, and 10 μM
Incubation Time 24 h
Method

HEK293T cells are treated with TD-158, TD-165, TD-343 or TD-487 (0.1, 1, and 10μM) for 24h, and VHL protein levels are analyzed by immunoblotting.

In Vivo
In vivo

TD-165 do not affect CRBN levels in the spleen, peripheral blood mononuclear cells (PBMCs), or liver of mice by immunoblotting, which might be attributable to the high plasma protein binding of TD-165. [1]

Chemical Information & Solubility

Molecular Weight 870.07 Formula

C46H59N7O8S

CAS No. 2305936-56-3 SDF --
Smiles CC1=C(SC=N1)C2=CC=C(CNC(=O)C3CC(O)CN3C(=O)C(NC(=O)CCCCCCCCCCNC4=C5C(=O)N(C6CCC(=O)NC6=O)C(=O)C5=CC=C4)C(C)(C)C)C=C2
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (114.93 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble


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In vivo
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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 ddH2O, 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.
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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