PBX-7016
Based on 1 Customer Validation
PBX-7016 is a DNA topoisomerase I inhibitor and DDX5 degrader. PBX-7016 induces DNA damage and downregulates Survivin, Mcl-1, and XIAP. PBX-7016 exerts a bystander killing effect. PBX-7016 can serve as an ADC payload for the synthesis of ADC. PBX-7016 is applicable to research related to head and neck cancer, non-small cell lung cancer, breast cancer, colorectal cancer, and ovarian cancer.
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- Pureza : 99.20%
- No. CAS: 3003834-34-9
- Fòrmula: C27H25N3O8
- Peso molecular:519.50
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Almacenamiento:
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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Actividad biológica
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Chemical Information
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
Topoisomerase I |
Mcl-1 |
XIAP |
In Vitro
PBX-7016 (72 h) potently inhibits the proliferation of A549 and FaDu cancer cell lines, with IC50 values of 16.3 nM and 1.07 nM respectively after 72 h of incubation[2].
PBX-7016 (10-100 nM; 24 h) dose-dependently downregulates the expression of anti-apoptotic proteins (Mcl-1, XIAP, DDX5, Survivin) in FaDu cells (following incubation at concentrations of 10 nM and 100 nM for 24 h)[2].
PBX-7016 (72 h) potently inhibits the proliferation of KPL-4, MDA-MB-453 and MDA-MB-468 breast cancer cell lines, and exhibits low cytotoxicity in normal NHEK cells; after 72 h of incubation, its IC50 is 223 nM[2].
PBX-7016 exhibits favorable in vitro ADME profiles and safety properties, including low CYP inhibition potential, no hERG-related cardiotoxicity risk, no phototoxicity, no genotoxicity, and metabolic stability across multiple species[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:FaDu (human head and neck squamous cell carcinoma)
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Concentration:10-100 nM
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Incubation Time:24 h
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Result:Induced dose-dependent downregulation of antiapoptotic proteins including Mcl-1, XIAP, DDX5, and Survivin, mirroring the activity of FL118.
In Vivo
The ADC Tra-LP1 (administered intravenously at 3-10 mg/kg) conjugated with PBX-7016 exhibits dose-dependent antitumor activity in nude mice bearing NCI-N87 gastric cancer xenografts, with a TGI of 43.0% at 3 mg/kg and 114.4% at 10 mg/kg, and no significant body weight loss is observed[2].
Nim-LP1 (5 mg/kg; intravenous injection; once weekly for 2 weeks), an EGFR-targeting ADC conjugated with PBX-7016, exhibits potent, target-specific anti-tumor activity in nude mice bearing EGFR-positive MDA-MB-468 breast cancer xenografts, with a TGI of 115.8%, and no significant body weight loss is observed[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude mice[2]
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Dosage:3 mg/kg; 10 mg/kg
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Administration:i.v.; once weekly; 2 weeks
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Result:Achieved a tumor growth inhibition (TGI) value of 65.5% (p < 0.001) at 3 mg/kg.
Achieved a tumor growth inhibition (TGI) value of 79.5% (p < 0.001) at 10 mg/kg.
Showed no observable body weight loss, animal deaths, or signs of systemic toxicity during the study.
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Animal Model:Nude mice[2]
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Dosage:3 mg/kg; 10 mg/kg
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Administration:i.v.
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Result:Achieved a TGI of 43.0% at 3 mg/kg, which was slightly more pronounced than the TGI of 30.2% for the control ADC.
Achieved a TGI of 114.4% at 10 mg/kg, which was greater than the TGI of 107.3% for the control ADC.
Showed no significant body weight loss in the treatment group.
Chemical Information
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No. CAS 3003834-34-9
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Appearance Solid
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Peso molecular 519.50
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Fòrmula C27H25N3O8
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Color Off-white to light yellow
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SMILES
C[C@@H](O)C(N[C@@H]1C2=C3C(CC1)=C4C(OCO4)=CC3=NC5=C2CN6C5=CC7=C(COC([C@]7(O)CC)=O)C6=O)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Pureza y Documentación
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Ficha de datos (283 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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Instrucciones de manejo (2659 KB)
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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