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.
For research use only. We do not sell to patients.
- CAS No.: 3003834-34-9
- Formula: C27H25N3O8
- Molecular Weight:519.50
-
Storage:
-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)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Protocols
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
Description
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. Further protocols information, click here.
-
Cell Line:FaDu (human head and neck squamous cell carcinoma)
-
Concentration:10-100 nM
-
Incubation Time:24 h
-
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.
-
Animal Model:BALB/c nude mice[2]
-
Dosage:3 mg/kg; 10 mg/kg
-
Administration:i.v.; once weekly; 2 weeks
-
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.
-
Animal Model:Nude mice[2]
-
Dosage:3 mg/kg; 10 mg/kg
-
Administration:i.v.
-
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
-
CAS No. 3003834-34-9
-
Appearance Solid
-
Molecular Weight 519.50
-
Formula C27H25N3O8
-
Color Off-white to light yellow
-
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
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
-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)
Protocols
-
Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.
-
Genotoxicity/Mutagenicity Study
The bacterial reverse mutation assay detects point mutations that restore amino-acid prototrophy in auxotrophic Salmonella typhimurium or Escherichia coli tester strains; after exposure to a test article, mutagenic activity is read out as an increased number of revertant colonies on minimal agar compared with the vehicle control. The assay uses tester strains with different mutation targets so that base-substitution and frameshift mutagens can be detected, and testing is performed with and without exogenous mammalian metabolic activation because some chemicals require biotransformation to become mutagenic.
Purity & Documentation
-
Data Sheet (283 KB)
-
SDS (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)
-
Handling Instructions (2659 KB)
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PBX-7016 Related Classifications
HY-178226 Related Classifications
Powered by Bioz