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Homo-PROTAC cereblon degrader 1 E3 Ligase inhibitor

Name: Homo-PROTAC cereblon degrader 1
Brand: Selleck Chemicals
SKU: S2881
Availability: InStock
Rating: 5 (2 reviews)

Cat.No.S2881

Homo-PROTAC cereblon degrader 1 (OUN20985) is a potent and efficient cereblon (CRBN) degrader with minimal effects on IKZF1 and IKZF3.

Chemical Structure

Molecular Weight: 660.63

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S288101 DMSO]100 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.51%

99.51

Related Targets	DUB Proteasome E1 Activating p97 SUMO E2 conjugating
Related Products	Skp2 inhibitor C1 (SKPin C1) PRT4165 Avadomide (CC-122) Apcin SZL P1-41 Mezigdomide (CC-92480)

Chemical Information, Storage & Stability

Molecular Weight	660.63	Formula	C₃₂H₃₂N₆O₁₀	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	2244520-98-5	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent

Solubility

In vitro
Batch:

DMSO : 100 mg/mL ( (151.37 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.500mg/ml (3.78mM)	Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

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.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

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 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.
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.

Mechanism of Action

Targets/IC₅₀/Ki	CRBN ^[1]
In vitro	Homo-PROTAC cereblon degrader 1 (OUN20985), a highly potent and efficient Cereblon (CRBN) degrader with only minimal effects on pomalidomide neosubstrates IKZF1 and IKZF3, has no effects on proliferation of different cell lines, prevents pomalidomide-induced degradation of IKZF1 and IKZF3, and antagonizes the effects of pomalidomide on multiple myeloma cellslidomide resistance in different multiple myeloma cells.^[1]
References	https://pubmed.ncbi.nlm.nih.gov/30118587/

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