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XZ739

Catalog No.GC61384

XZ739, a Cereblon-dependent PROTAC BCL-XL (Bcl-2 family member) 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.

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XZ739 Chemical Structure

Cas No.: 2365172-19-4

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5mg
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10mg
$2,364.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

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].

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

[1]. Xuan Zhang,et al. Discovery of PROTAC BCL-X L Degraders as Potent Anticancer Agents With Low On-Target Platelet Toxicity. Eur J Med Chem. 2020 Apr 15;192:112186.

Chemical Properties

Cas No. 2365172-19-4 SDF
Canonical 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
Formula C65H76ClF3N8O12S3 M.Wt 1349.99
Solubility DMSO: 20 mg/mL (14.81 mM) Storage -20°C, stored under nitrogen
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 0.7407 mL 3.7037 mL 7.4075 mL
5 mM 0.1481 mL 0.7407 mL 1.4815 mL
10 mM 0.0741 mL 0.3704 mL 0.7407 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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Reviews

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Average Rating: 5 ★★★★★ (Based on Reviews and 37 reference(s) in Google Scholar.)

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