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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 2894135-13-6
- 分子式: C19H21N3O9
- 分子量:435.38
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
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 |
体外実験
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 |
体内実験
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%.
化学情報
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CAS 番号 2894135-13-6
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分子量 435.38
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Pomalidomide-β-D-glucose 関連分類
HY-189288 関連分類
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