2. PROTAC
    Apoptosis
  3. Ligands for E3 Ligase
    Apoptosis
    Molecular Glues
  4. Iberdomide

Iberdomide  (Synonyms: CC-220)

Cat. No.: HY-101291 Purity: 98.84%
COA Handling Instructions

Iberdomide (CC-220) est un modulateur de cereblon (CRBN) avec une valeur IC50 de 60 nM.

Iberdomide (CC-220) is an orally active and potent cereblon (CRBN) E3 ligase modulator (CELMoD) with an IC50 of ~150 nM for cereblon-binding affinity. Iberdomide, a derivative of Thalidomide (HY-14658), has antitumor and immunostimulatory activities.

For research use only. We do not sell to patients.

Iberdomide Chemical Structure

Iberdomide Chemical Structure

CAS No. : 1323403-33-3

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10 mM * 1 mL in DMSO USD 119 In-stock
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Based on 7 publication(s) in Google Scholar

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Iberdomide (CC-220) is an orally active and potent cereblon (CRBN) E3 ligase modulator (CELMoD) with an IC50 of ~150 nM for cereblon-binding affinity. Iberdomide, a derivative of Thalidomide (HY-14658), has antitumor and immunostimulatory activities[1][2].

In Vitro

Iberdomide (CC-220; 0.01, 0.1, 1, 10 μM; 72-96 hrs) has antiproliferative effects in a panel of multiple myeloma (MM) cell lines (EJM, H929, KMS11, KMS128M, KMS12PE, MM1.S, MM1.R, RPM-8226, U266 cells) across a range of concentrations[1].
Iberdomide (0.1 μM; 96 hrs) induces apoptosis in all MM cell lines[1].
Iberdomide (0.1 μM; 24, 48, 72 hrs) results in time-dependent increases in G0/G1 and sub-G1 cell cycle fractions on H929 cells[1].
Iberdomide leads to rapid Aiolos depletion in the KMS12BM line[1].
Iberdomide (0.1 μM) displays some anti-proliferative activity in two of the Pomalidomide-resistant (PR) lines with cereblon mutations (EJM/PR and H929/PR) along with decreased levels of cereblon protein[1].
Iberdomide (0.1-1000 nM; 72 hrs) equally induces PBMC-mediated killing of both parental MM1.S cells and MM1.S/PR cells[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo

Iberdomide (CC-220; 10 mg/kg; oral gavage) after 6 or 24 hours causes higher hCRBN expression in hC343 splenocytes correlated to deeper IKZF1/3 downregulation in WT (C57BL/6), hC123, or-343, (representing two different transgenic founder lines expressing hCRBN) and mCrbn-/- mice[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

449.50

Appearance

Solid

Formula

C25H27N3O5
CAS No.
SMILES

O=C([[email protected]@H](N(CC1=C2C=CC=C1OCC3=CC=C(CN4CCOCC4)C=C3)C2=O)CC5)NC5=O
Shipping

Room temperature in continental US; may vary elsewhere.
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 : 125 mg/mL (278.09 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2247 mL 11.1235 mL 22.2469 mL
5 mM 0.4449 mL 2.2247 mL 4.4494 mL
10 mM 0.2225 mL 1.1123 mL 2.2247 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.63 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.63 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.63 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 98.84%

COA (252 KB) HNMR (277 KB) LCMS (245 KB)

Handling Instructions (2659 KB)
References
Kinase Assay
[1]

Iberdomide is dissolved in DMSO. In the assay, 60 nM 6Xhis-tagged CRBN-DDB1 is combined with 30 nM cy5-conjugated cereblon modulator and 3 nM LanthaScreen Eu-anti-His Tag antibody in 20 mM HEPES pH 7, 150 mM NaCl, 0.005% Tween-20 assay buffer. FRET is observed by exciting at 340 nm and monitoring emission at 615 nm and 665 nm, and FRET efficiency is determined by the ratio of FRET to non-FRET emission. Competing cereblon modulating compound (Iberdomide) or DMSO carrier is titrated and incubated for 10 min before scanning[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

Iberdomide1323403-33-3CC-220CC220CC 220Ligands for E3 LigaseApoptosisMolecular GluesE3 ligase-recruiting MoietyorallycereblonCRBNE3ligaseCELMoDThalidomidemultiplemyelomaEJMH929KMS11KMS128MKMS12PEMM1.SMM1.RRPM-8226U266G0/G1sub-G1Inhibitorinhibitorinhibit

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