ABT-002
ABT-002 is a molecular glue degrader targeting GSPT1 and NEK7. ABT-002 is the active metabolite of ABS-752 (HY-W599279). ABT-002 directly binds the E3 ubiquitin ligase complex component CRBN and the neo-substrates (GSPT1 and NEK7) to form a stable CRBN-substrate ternary complex, thereby inducing ubiquitination and degradation of the target proteins and triggering subsequent cytotoxicity and antitumor effects. ABT-002 can be used for research on hepatocellular carcinoma.
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- No. CAS: 2438239-83-7
- Fòrmula: C14H11FN2O5
- Peso molecular:306.25
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Ver todos los productos específicos de isoformas Eukaryotic Release Factor (eRF)
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
NEK7 |
eRF3a/GSPT1 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Hep 3B2 | IC50 |
20.4 μM
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Absolute IC50 for viability reduction against wild-type Hep3B cells by CTG assay.
Absolute IC50 for viability reduction against wild-type Hep3B cells by CTG assay.
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40813917 |
In Vitro
ABT-002 (2 nM-50 μM) exhibits activity in inducing the formation of GSPT1-CRBN and NEK7-CRBN ternary complexes in the TR-FRET ternary complex formation assay[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | C0 | Vd | Clearance (CL) | AUCinf |
|---|---|---|---|---|---|---|
| Mice[1] | 1 mg/kg | i.v. | 4920 ng/mL | 1.9 L/kg | 36.2 mL/min/kg | 548 ng·h/mL |
Chemical Information
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No. CAS 2438239-83-7
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Peso molecular 306.25
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Fòrmula C14H11FN2O5
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SMILES
O=C1CCC(C(N1)=O)N2CC3=C(C2=O)C=C(C(C(O)=O)=C3)F
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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)
ABT-002 Related Classifications
HY-175283 Related Classifications
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