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    Bcl-2 Family
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  3. XZ739

XZ739 

目录号: HY-133557
产品使用指南

XZ739 是一种基于 CRBN 的 PROTAC BCL-XL 降解剂,作用于 MOLT-4 细胞,处理 16 小时后,DC50 值为 2.5 nM。XZ739 还通过 caspase 介导的凋亡 (apoptosis) 诱导细胞死亡。

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XZ739 Chemical Structure

XZ739 Chemical Structure

CAS No. : 2365172-19-4

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Description

XZ739, a CRBN-dependent PROTAC BCL-XL degrader with a DC50 value of 2.5 nM in MOLT-4 cells after 16 h treatment. XZ739 also induces cell death through caspase-mediated apoptosis[1].

IC50 & Target[1]

Cereblon

 

Bcl-xL

2.5 nM (DC50)

In Vitro

XZ739 (0.001-10 μM; 48 hours) potently reduces the viability of T-ALL MOLT-4, B-ALL RS4; 11, SCLC NCI-H146 cells, and platelets after 48 h treatment with IC50s of 10.1, 41.8, 25.3, and 1217 nM, respectively. XZ739 has >100-fold selectivity for MOLT-4 cells over human platelets[1].
XZ739 (1.2-300 nM; 16 hours) induces BCL-XL degradation in MOLT-4 cells[1].
The BCL-XL degradation induced by XZ739 in MOLT-4 is rapid, starting within 2 h; and 8 h after XZ739 treatment, more than 96% of the BCL-XL is degraded with 100 nM of XZ739[1].

Cell Viability Assay[1]

Cell Line: Human platelets and MOLT-4 cells
Concentration: 0.001, 0.01, 0.1, 1, and 10 μM
Incubation Time: 48 hours
Result: IC50 values were 10.1 nM and 1217 nM for MOLT-4 cells and platelets, respectively.

Western Blot Analysis[1]

Cell Line: MOLT-4 cells
Concentration: 1.2, 3.7, 11, 33, 100, 300 nM
Incubation Time: 16 hours
Result: Dose-dependently induced BCL-XL degradation.
Molecular Weight

1349.99

Formula

C₆₅H₇₆ClF₃N₈O₁₂S₃

CAS No.

2365172-19-4

SMILES

O=C(C1=CC=C(N2CCN(CC3=C(C4=CC=C(Cl)C=C4)CCC(C)(C)C3)CC2)C=C1)NS(C5=CC(S(=O)(C(F)(F)F)=O)=C(N[C@@H](CSC6=CC=CC=C6)CCN(C)CCOCCOCCOCCNC7=C8C(C(N(C9CCC(NC9=O)=O)C8=O)=O)=CC=C7)C=C5)(=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

XZ739XZ 739XZ-739PROTACBcl-2 FamilyApoptosisProteolysis-targeting chimeraCRBNMOLT-4PlateletDegradationB-ALLRS411SCLCNCI–H146H146Inhibitorinhibitorinhibit

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