2. PROTAC
  3. Ligands for E3 Ligase Molecular Glues
  4. Golcadomide

Golcadomide (CC-99282) is a potent and orally active CRBN E3 ligase modulator (CELMoD). Golcadomide interacts with the CRL4 CRBN E3 ubiquitin ligase substrate receptor CRBN, inducing the recruitment and ubiquitin-mediated proteasomal degradation of the transcription factors Ikaros and Aiolos. Golcadomide shows potential for research in cancer-related fields, including chronic lymphocytic leukemia (CLL) and non-Hodgkin lymphoma (NHL).

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Golcadomide

Golcadomide Estructura química

No. CAS : 2379572-34-4

Tamaño Precio Stock Cantidad
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
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Golcadomide Related Antibodies

Top Publications Citing Use of Products

Ver todos los productos específicos de isoformas Ligands for E3 Ligase:

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von Hippel-Lindau (VHL) MDM2 Cereblon IAP KLHDC2 Fbxo3 RNF4 DCAF11 DCAF1 UHRF1 TRIM21 NEURL1B KLHL41

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Descripciòn

Golcadomide (CC-99282) is a potent and orally active CRBN E3 ligase modulator (CELMoD). Golcadomide interacts with the CRL4 CRBN E3 ubiquitin ligase substrate receptor CRBN, inducing the recruitment and ubiquitin-mediated proteasomal degradation of the transcription factors Ikaros and Aiolos. Golcadomide shows potential for research in cancer-related fields, including chronic lymphocytic leukemia (CLL) and non-Hodgkin lymphoma (NHL)[1][2].

IC50 & Target[1]

Cereblon

 

In Vivo

Golcadomide (1 mg/kg) monotherapy results in modest tumor growth inhibition, whereas the combination of Golcadomide (1 mg/kg) and rituximab (10 mg/kg) results in tumor regression in 100% of animals in the WSU-DLCL2 model and the FL xenograft model.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Ensayo clínico
Peso molecular

535.57

Fòrmula

C28H30FN5O5
No. CAS
Appearance

Solid

Color

Light yellow to yellow

SMILES

FC(C=C(C=C1)CN2CC(N3CCOCC3)C2)=C1CNC4=C5C(C(N([C@]6([H])C(NC(CC6)=O)=O)C5=O)=O)=CC=C4
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvente y solubilidad
In Vitro: 

DMSO : 125 mg/mL (233.40 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8672 mL 9.3358 mL 18.6717 mL
5 mM 0.3734 mL 1.8672 mL 3.7343 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Calculadora de molaridad

  • Calculadora de dilución

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Pureza y Documentación
Referencias

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8672 mL 9.3358 mL 18.6717 mL 46.6792 mL
5 mM 0.3734 mL 1.8672 mL 3.7343 mL 9.3358 mL
10 mM 0.1867 mL 0.9336 mL 1.8672 mL 4.6679 mL
15 mM 0.1245 mL 0.6224 mL 1.2448 mL 3.1119 mL
20 mM 0.0934 mL 0.4668 mL 0.9336 mL 2.3340 mL
25 mM 0.0747 mL 0.3734 mL 0.7469 mL 1.8672 mL
30 mM 0.0622 mL 0.3112 mL 0.6224 mL 1.5560 mL
40 mM 0.0467 mL 0.2334 mL 0.4668 mL 1.1670 mL
50 mM 0.0373 mL 0.1867 mL 0.3734 mL 0.9336 mL
60 mM 0.0311 mL 0.1556 mL 0.3112 mL 0.7780 mL
80 mM 0.0233 mL 0.1167 mL 0.2334 mL 0.5835 mL
100 mM 0.0187 mL 0.0934 mL 0.1867 mL 0.4668 mL
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Golcadomide Related Classifications

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.

Keywords:

Golcadomide2379572-34-4CC-99282CC99282CC 99282Ligands for E3 LigaseMolecular GluesE3 ligase-recruiting Moietyorally activenon-Hodgkin lymphomasIkarosAiolosCRBNInhibitorinhibitorinhibit

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Nombre del producto:
Golcadomide
Cat. No.:
HY-146237
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