2. PROTAC Apoptosis
  3. PROTACs Bcl-2 Family Apoptosis
  4. PZ671

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). (Structure Note: Pink: Bcl-xL ligand (HY-174878); Blue: CRBN Ligand (HY-138793); Black: linker; E3-linker (HY-174879))

For research use only. We do not sell to patients.

PZ671

PZ671 Chemical Structure

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Customer Review

Based on 1 publication(s) in Google Scholar

PZ671 Related Antibodies

Top Publications Citing Use of Products

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

  • Biological Activity

  • Purity & Documentation

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Description

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)[1]. (Structure Note: Pink: Bcl-xL ligand (HY-174878); Blue: CRBN Ligand (HY-138793); Black: linker; E3-linker (HY-174879))

IC50 & Target[1]

Bcl-xL

 

Cereblon

 

In Vitro

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.

PZ671 Related Antibodies

Western Blot Analysis[1]

Cell Line: MOLT-4 cells
Concentration: 0.4, 1, 3, 11, 33. and 100 nM
Incubation Time: 16 h, and 100 nM for 1, 2, 3, 4, 5, 6 h
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.

Western Blot Analysis[1]

Cell Line: MOLT-4 cells
Concentration: 10 and 100 nM, pretreatingt with 1 μM MG-132 (HY-13259) for 2 h
Incubation Time: /
Result: Degradation was blocked by proteasome inhibitor MG-132 (HY-13259).

Western Blot Analysis[1]

Cell Line: MOLT-4 cells
Concentration: 0.4, 1, 3, 11, 33. and 100 nM
Incubation Time: 16 h
Result: Dose-dependently increased poly (ADP-ribose) polymerase (PARP) and caspase-3 cleavage.
Significantly reduced β-actin levels with increasing concentrations.

Western Blot Analysis[1]

Cell Line: Human platelets
Concentration: 30, 100, 300 and 1000 nM
Incubation Time: 48 h
Result: Degraded Bcl-xL at concentrations above 1 μM.
In Vivo

PZ671 (1.5 mg/kg/, i.p., q4d for 22 days) markedly suppresses the tumor growth but induces only a transient drop in platelet counts following its administration with rapid recovery from thesecond day onwards in MOLT-4 xenograft mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: MOLT-4 xenograft mice (CB-17 SCID, Female, 5-6 weeks)[1]
Dosage: 1.5 mg/kg
Administration: Intraperitoneal injection, every 4 days for 22 days
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.
Molecular Weight

1335.02

Formula

C66H79ClF3N7O11S3
Appearance

Solid

Color

Off-white to light yellow

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.7491 mL 3.7453 mL 7.4905 mL
5 mM 0.1498 mL 0.7491 mL 1.4981 mL
View the 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

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C2

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Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
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
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
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PZ671 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PZ671PZ 671PZ-671PROTACsBcl-2 FamilyApoptosisBcl-xLSmall cell lung cancerMOLT-4 cellsMOLT-4 xenograft miceInhibitorinhibitorinhibit

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