ABS-752 hydrochloride
Based on 1 Customer Validation
ABS-752 is an orally active prodrug of CRBN-modulating molecular glue targeting. ABS-752 can effectively degrade GSPT1. ABS-752 can degrade NEK7. ABS-752 does not form ternary complexes with CRBN and the neosubstrates. ABS-752 is a prodrug activated by the monoamine oxidase, VAP-1, to an aldehyde intermediate and subsequently to the active molecule, ABT-002. ABS-752 can be used for the study of hepatocellular carcinoma (HCC).
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.81%
- CAS. Nr.: 2922884-90-8
- Formel: C14H15ClFN3O3
- Molecular Weight:327.74
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Speicherung:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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Biologische Aktivität
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NEK7 |
GSPT1 |
ABS-752 (6-24 h) degrades GSPT1, NEK7, CK1α in Hep3B cells and SALL4 in Kelly cells, but does not degrade IKZF1 in H929 cells[1].
ABS-752 (0.01-10 μM, 48-72 h) exerts its cytotoxicity to Hep3B cells mainly through GSPT1[1].
ABS-752 (0.1-10 μM, 24 h) can induce NEK7 degradation in Hep3B wild-type cells, and this degradation still occurs in the G575N mutant[1].
ABS-752’s (0.1 nM-30 μM, 72 h) activity and target protein downregulation in Hep3B and KG-1 cell lines are abolished by PXS-4728A[1].
ABS-752 (0.1 nM-30 μM, 72 h) significantly reduces Hep3B and KG-1 viability in FBS-supplemented medium, but not in human serum-supplemented medium[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Hep3B cells, G575N mutant Hep3B cells
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Concentration:0.01 μM, 0.1 μM, 1 μM, 10 μM
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Incubation Time:48 h
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Result:In G575N mutant Hep3B cells, GSPT1 is not degraded; however, in wild-type Hep3B cells, GSPT1 is effectively degraded.
ABS-752 (100 mg/kg, p.o., twice daily for 20-21 days) effectively inhibits tumor growth in a human hepatocellular carcinoma patient-derived liver cancer xenograft mouse model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female NSG mice subcutaneously implanted with Hep3B human liver cancer cell line[1].
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Dosage:1 mg/kg, 3 mg/kg, 10 mg/kg
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Administration:P.o., twice daily for 14 days
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Result:The 10 mg/kg group showed complete tumor regression.
The 3 mg/kg and 1 mg/kg groups showed significant and moderate tumor growth inhibition, respectively.
GSPT1 and NEK7 degradation was observed in the tumor samples.
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Animal Model:10 Subcutaneous patient-derived liver cancer xenograft (PDX) models were developed in female BALB/c nude mice[1].
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Dosage:100 mg/kg
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Administration:P.o., twice daily for 20-21 days
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Result:Of the 10 PDX models, 8 showed tumor growth inhibition, with 4 of them having a TGI >50%.
Chemical Information
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CAS. Nr. 2922884-90-8
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Appearance Solid
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Molecular Weight 327.74
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Formel C14H15ClFN3O3
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Color White to off-white
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SMILES
O=C1C2=CC(F)=C(CN)C=C2CN1C3C(NC(CC3)=O)=O.Cl
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Lösungsmittel & Löslichkeit
DMSO : 25 mg/mL (76.28 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
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 (sealed storage, away from moisture). 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 | 3.0512 mL | 15.2560 mL | 30.5120 mL | 76.2800 mL |
| 5 mM | 0.6102 mL | 3.0512 mL | 6.1024 mL | 15.2560 mL | |
| 10 mM | 0.3051 mL | 1.5256 mL | 3.0512 mL | 7.6280 mL | |
| 15 mM | 0.2034 mL | 1.0171 mL | 2.0341 mL | 5.0853 mL | |
| 20 mM | 0.1526 mL | 0.7628 mL | 1.5256 mL | 3.8140 mL | |
| 25 mM | 0.1220 mL | 0.6102 mL | 1.2205 mL | 3.0512 mL | |
| 30 mM | 0.1017 mL | 0.5085 mL | 1.0171 mL | 2.5427 mL | |
| 40 mM | 0.0763 mL | 0.3814 mL | 0.7628 mL | 1.9070 mL | |
| 50 mM | 0.0610 mL | 0.3051 mL | 0.6102 mL | 1.5256 mL | |
| 60 mM | 0.0509 mL | 0.2543 mL | 0.5085 mL | 1.2713 mL |
ABS-752 hydrochloride Related Classifications
HY-W998347 Related Classifications
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