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Iberdomide (CC220) E3 ligase Ligand chemical

Name: Iberdomide (CC220)
Brand: Selleck Chemicals
SKU: S8760
Availability: InStock
Rating: 5 (11 reviews)

Cat.No.S8760

Iberdomide (CC-220) is a novel oral immunomodulatory compound that targets cereblon, part of the CRL4CRBN E3 ubiquitin ligase complex, with an IC50 of 60 nM in a competitive TR-FRET assay. This compound induces apoptosis with antitumor and immunostimulatory activities.

Chemical Structure

Molecular Weight: 449.50

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

Quality Control

Batch: Purity: 99.75%

99.75

Related Targets	Immunology & Inflammation related CD markers Interleukins Anti-infection Antioxidant COX Histamine Receptor TNF-alpha ROS Parasite PD-1/PD-L1 TLR Prostaglandin Receptor IFN CXCR Nrf2 NOS CCR NLRP3 eIF STING AhR IL Receptor Complement System IRAK β-lactamase IDO/TDO PGES NADPH-oxidase FKBP

Chemical Information, Storage & Stability

Molecular Weight	449.50	Formula	C₂₅H₂₇N₃O₅	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1323403-33-3	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1CC(=O)NC(=O)C1N2CC3=C(C2=O)C=CC=C3OCC4=CC=C(C=C4)CN5CCOCC5

Solubility

In vitro
Batch:

DMSO : 90 mg/mL ( (200.22 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 5 mg/mL

Water : 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.
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.
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.

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	cereblon ^[1] 60 nM
In vitro	Iberdomide (CC-220) is a potent anti-proliferative and pro-apoptotic compound that shows activity in several MM cell line categories. In cellular degradation assays, treatment with this compound results in the loss of Ikaros protein levels with an EC50 of 1 nM. It is similarly potent toward Aiolos, with an EC50 of 0.5 nM^[1]. It induces PBMC-mediated killing of all MM cell lines regardless of the level of Cereblon expression and cell autonomous sensitivity. This compound acts through binding of Cereblon, leading to the degradation of the hematopoietic transcription factors Ikaros and Aiolos, followed by disruption of the MM promoting c-Myc/IRF4 axis^[2].
References	https://pubmed.ncbi.nlm.nih.gov/28425720/ http://www.bloodjournal.org/content/128/22/1591?sso-checked=true https://pubmed.ncbi.nlm.nih.gov/34258584/

Applications

Methods	Biomarkers	Images	PMID
Western blot	Aiolos / Ikaros IKZF1 / IKZF3 / ZFP91 / CK1α / CBRN / UBE2G1		28848067

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT06216158	Recruiting	Multiple Myeloma	University of Heidelberg Medical Center\|KKS Netzwerk\|Wuerzburg University Hospital\|Sanofi\|Bristol-Myers Squibb	April 5 2024	Phase 3
NCT06215118	Recruiting	Multiple Myeloma	Pfizer\|Bristol-Myers Squibb	February 20 2024	Phase 1
NCT05827016	Recruiting	Multiple Myeloma	Bristol-Myers Squibb	June 22 2023	Phase 3
NCT05560399	Enrolling by invitation	Multiple Myeloma	Icahn School of Medicine at Mount Sinai\|Multiple Myeloma Research Consortium\|Bristol-Myers Squibb	February 6 2023	Early Phase 1

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Handling Instructions

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