PZ671
Based on 1 Customer Validation
PZ671 is a Bcl-xL PROTAC degrader that recruits cereblon, with a DC50 of 0.9 nM in MOLT-4 T-ALL cells. PZ671 induces apoptosis via activation of caspase-3 and cleavage of PARP, and exhibits antitumor activity in T-cell acute lymphoblastic leukemia and small cell lung cancer models. PZ671 can be used for the research of T-cell acute lymphoblastic leukemia and small cell lung cancer.
(Pink: Bcl-xL ligand (HY-174878); Blue: Cereblon ligand (HY-138793); Black: linker).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 98.70%
- Fòrmula: C66H79ClF3N7O11S3
- Peso molecular:1335.02
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Almacenamiento: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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
Bcl-xL 0.9 nM (DC50) |
Caspase-3 |
PARP |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MOLT-4 | IC50 |
1.3 nM
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Reduction of MOLT-4 T-ALL cell viability incubated for 48 hrs by cell viability assay.
Reduction of MOLT-4 T-ALL cell viability incubated for 48 hrs by cell viability assay.
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40510905 |
| MOLT-4 | DC50 |
0.9 nM
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Induction of dose-dependent Bcl-xL degradation in MOLT-4 T-ALL cells incubated for 16 hrs by immunoblotting-based protein degradation assay.
Induction of dose-dependent Bcl-xL degradation in MOLT-4 T-ALL cells incubated for 16 hrs by immunoblotting-based protein degradation assay.
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40510905 |
| Platelet | IC50 |
32 nM
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Reduction of human platelet viability incubated for 48 hrs by cell viability assay.
Reduction of human platelet viability incubated for 48 hrs by cell viability assay.
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40510905 |
In Vitro
PZ671 (48 h) (compound 5b) potently reduces the viability of MOLT-4 T-ALL cells, with an IC50 of 1.3 nM[1].
PZ671 (0.1-100 nM; 16 h) induces proteasome-dependent Bcl-xL degradation in MOLT-4 T-ALL cells, with a DC50 of 0.9 nM[1].
PZ671 (30-1000 nM; 48 h) reduces human platelet activity with an IC50 of 32 nM, and is 25-fold more selective for MOLT-4 T-ALL cells than for platelets[1].
PZ671 potently inhibits the proliferation of MOLT-4 T-cell acute lymphoblastic leukemia cells, with an IC50 of 1.3 nM[2].
PZ671 (0.4-100 nM; 16 h) induces caspase-dependent apoptosis in MOLT-4 T-ALL cells, as evidenced by increased levels of cleaved PARP and cleaved caspase-3, as well as an increase in annexin V-positive apoptotic cells, whereas pretreatment with Q-VD-OPh (QVD) (HY-12305) reverses this increase in apoptotic cells[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 T-ALL cells
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Concentration:0.4, 1, 3, 11, 33, 100 nM
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Incubation Time:16 h; 1, 2, 3, 4, 5, 6 h
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Result:Induced dose-dependent degradation of Bcl-xL with a DC50 of 0.9 nM.
Showed an ~6-fold enhancement in degradation potency compared to XZ739.
Blocked Bcl-xL degradation with proteasome inhibitor MG-132 pretreatment, confirming a proteasome-dependent mechanism.
Significantly reduced Bcl-xL levels within 2 h of 100 nM treatment.
Achieved almost complete Bcl-xL degradation by 4 h of 100 nM treatment.
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Cell Line:MOLT-4 T-ALL cells
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Concentration:0.4, 1, 3, 11, 33, 100 nM
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Incubation Time:16, 24 h
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Result:Dose-dependently increased levels of cleaved PARP and cleaved caspase-3, indicating apoptotic cell death induction.
Significantly increased the percentage of apoptotic cells at 10 nM treatment.
Attenuated apoptotic effect with pan-caspase inhibitor QVD pretreatment.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CB-17 SCID (5 weeks old; subcutaneously implanted with 5×106 MOLT-4 cells mixed 1:1 with Matrigel)[1]
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Dosage:1.5 mg/kg
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Administration:i.p.; every 4 days
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Result:Markedly suppressed MOLT-4 xenograft tumor growth.
Caused a transient ~72% reduction in platelet counts 1 day post-administration, with rapid platelet recovery starting on day 2.
Chemical Information
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Appearance Solid
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Peso molecular 1335.02
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Fòrmula 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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
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)
Pureza y Documentación
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Ficha de datos (279 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
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 |
|---|---|---|---|---|---|
| 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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