PZ671
Based on 1 Customer Validation
PZ671 is a potent Bcl-xL PROTAC degrader with an IC50 of 1.3 nM (MOLT-4 cells) and a DC50 of 0.9 nM (Bcl-xL). PZ671 induces apoptosis in MOLT-4 cells. PZ671 effectively inhibits tumor growth and rapidly reverses transient platelet counts reduction in MOLT-4 xenograft mice. PZ671 can be used for the research of cancer, such as small cell lung cancer (SCLC).
(Pink: Bcl-xL ligand (HY-174878); Blue: Cereblon ligand (HY-138793); Black: linker).
For research use only. We do not sell to patients.
- Purity: 98.70%
- Formula: C66H79ClF3N7O11S3
- Molecular Weight:1335.02
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
All PROTACs Isoforms
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Biological Activity
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Bcl-xL |
Cereblon |
PZ671 (Compound 5b) (0.4-100 nM, 1-16 h) induces Bcl-xL degradation in MOLT-4 cells[1].
PZ671 (10, 100 nM) degrades Bcl-xL depending on proteasome in MOLT-4 cells[1].
PZ671 (0.4-100 nM, 48 h) induces apoptosis in MOLT-4 cells[1].
PZ671 (30-1000 nM, 48 h) degrades Bcl-xL at concentrations above 1 μM in human platelets[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MOLT-4 cells
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Concentration:0.4, 1, 3, 11, 33. and 100 nM
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Incubation Time:16 h, and 100 nM for 1, 2, 3, 4, 5, 6 h
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Result:Induced dose-dependent Bcl-xL degradation in MOLT-4 cells.
Significantly reduced Bcl-xL levels within 2 h, and almost complete degradation of Bcl-xL after 4 h at 100 nM.
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Cell Line:MOLT-4 cells
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Concentration:10 and 100 nM, pretreatingt with 1 μM MG-132 (HY-13259) for 2 h
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Incubation Time:/
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Result:Degradation was blocked by proteasome inhibitor MG-132 (HY-13259).
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Cell Line:MOLT-4 cells
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Concentration:0.4, 1, 3, 11, 33. and 100 nM
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Incubation Time:16 h
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Result:Dose-dependently increased poly (ADP-ribose) polymerase (PARP) and caspase-3 cleavage.
Significantly reduced β-actin levels with increasing concentrations.
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Cell Line:Human platelets
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Concentration:30, 100, 300 and 1000 nM
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Incubation Time:48 h
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Result:Degraded Bcl-xL at concentrations above 1 μM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MOLT-4 xenograft mice (CB-17 SCID, Female, 5-6 weeks)[1]
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Dosage:1.5 mg/kg
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Administration:Intraperitoneal injection, every 4 days for 22 days
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Result:Markedly suppressed the tumor growth.
Caused a transient ∼72% reduction in platelet counts after a single dose, with rapid recovery from the second day onward.
Chemical Information
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Appearance Solid
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Molecular Weight 1335.02
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Formula C66H79ClF3N7O11S3
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Color Off-white to light yellow
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SMILES
O=C(NS(=O)(C1=CC=C(N[C@@H](CSC2=CC=CC=C2)CCN(C)CCOCCOCCOCCCC3=CC4=C(C(N(C(CC5)C(NC5=O)=O)C4)=O)C=C3)C(S(=O)(C(F)(F)F)=O)=C1)=O)C6=CC=C(N7CCN(CC8=C(C9=CC=C(Cl)C=C9)CCC(C)(C)C8)CC7)C=C6
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (74.91 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. 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (273 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)
References
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. 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 |
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| DMSO | 1 mM | 0.7491 mL | 3.7453 mL | 7.4905 mL | 18.7263 mL |
| 5 mM | 0.1498 mL | 0.7491 mL | 1.4981 mL | 3.7453 mL | |
| 10 mM | 0.0749 mL | 0.3745 mL | 0.7491 mL | 1.8726 mL | |
| 15 mM | 0.0499 mL | 0.2497 mL | 0.4994 mL | 1.2484 mL | |
| 20 mM | 0.0375 mL | 0.1873 mL | 0.3745 mL | 0.9363 mL | |
| 25 mM | 0.0300 mL | 0.1498 mL | 0.2996 mL | 0.7491 mL | |
| 30 mM | 0.0250 mL | 0.1248 mL | 0.2497 mL | 0.6242 mL | |
| 40 mM | 0.0187 mL | 0.0936 mL | 0.1873 mL | 0.4682 mL | |
| 50 mM | 0.0150 mL | 0.0749 mL | 0.1498 mL | 0.3745 mL | |
| 60 mM | 0.0125 mL | 0.0624 mL | 0.1248 mL | 0.3121 mL |
PZ671 Related Classifications
HY-174876 Related Classifications
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