Pomalidomide-β-D-glucose
Pomalidomide-β-D-glucose is an orally active Molecular glue degrader of IKZF1 and CK1α. Pomalidomide-β-D-glucose forms a ternary complex with CRBN and substrate proteins, inducing ubiquitination and proteasomal degradation of IKZF1 and CK1α. Pomalidomide-β-D-glucose undergoes GLUT1-mediated cellular uptake. Pomalidomide-β-D-glucose can be used for research on multiple myeloma.
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- No. CAS: 2894135-13-6
- Fòrmula: C19H21N3O9
- Peso molecular:435.38
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
GLUT1 |
IKZF1 |
CRBN |
CK1α |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| U-251 | IC50 |
4.77 μM
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Cytotoxicity against human U251 glioma cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
Cytotoxicity against human U251 glioma cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
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42561560 |
| MM1.S | IC50 |
4.55 μM
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Cytotoxicity against human MM.1S multiple myeloma cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
Cytotoxicity against human MM.1S multiple myeloma cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
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42561560 |
| MM1.S | IC50 |
21.22 μM
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Cytotoxicity against lenalidomide-resistant human MM.1S/LEN multiple myeloma cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
Cytotoxicity against lenalidomide-resistant human MM.1S/LEN multiple myeloma cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
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42561560 |
| MM1.S | IC50 |
13.97 μM
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Cytotoxicity against pomalidomide-resistant human MM.1S/POM multiple myeloma cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
Cytotoxicity against pomalidomide-resistant human MM.1S/POM multiple myeloma cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
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42561560 |
In Vitro
Pomalidomide-β-D-glucose (72 h) exhibits potent cytotoxicity against U251, MM.1S, and the lenalidomide- and pomalidomide-resistant MM.1S cell lines, with IC50 values of 4.77, 4.55, 21.22, and 13.97 μM, respectively[1].
Pomalidomide-β-D-glucose (1-25 μM) acts as a molecular glue degrader, inducing the degradation of IKZF1 and CK1α in both MM.1S/LEN and MM.1S/POM cells, and also degrades IKZF3 in MM.1S/LEN cells[1].
Pomalidomide-β-D-glucose (5-20 μM) cellular uptake in U251 cells is concentration-dependent and directly associated with the GLUT1-mediated transport channel[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | T1/2 | Tmax | Cmax | AUC0-t | AUC0-∞ | MRT |
|---|---|---|---|---|---|---|---|---|
| Mice[1] | 5 mg/kg | i.g. | 2.65 h | 0.25 h | 1607.13 ng/mL | 1543.18 ng·h/mL | 1772.31 ng·h/mL | 3.33 h |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD/SCID (female, 5-week-old, MM.1S/POM xenograft model)[1]
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Dosage:15 mg/kg
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Administration:p.o.; once daily; 14 days
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Result:Achieved a tumor volume-based TGI of 64.9%.
Achieved a tumor weight-based TGI of 60.5%.
Maintained a positive body weight gain of 10.9%.
Chemical Information
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No. CAS 2894135-13-6
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Peso molecular 435.38
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Fòrmula C19H21N3O9
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SMILES
O=C(NC1=O)CCC1N2C(C3=C(N[C@H]4[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O4)C=CC=C3C2=O)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pomalidomide-β-D-glucose Related Classifications
HY-189288 Related Classifications
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