XZ338
Based on 1 Customer Validation
XZ338 is a highly potent and selective BCL-XL PROTAC degrader derived from A-1331852 (HY-19741), with a DC50 of 0.43 nM in MOLT‑4 cells. XZ338 induces the formation of a ternary complex with BCL-XL and VHL E3 ligase, mediates target protein degradation via the ubiquitin-proteasome system, and exhibits significantly weaker degradation activity in platelets than in tumor cells. XZ338 possesses anti-cancer activity. XZ338 can be used in the research of T-cell acute lymphoblastic leukemia (T-ALL).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.17%
- Fòrmula: C69H83N11O8S3
- Peso molecular:1290.66
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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 0.43 nM (DC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MOLT-4 | IC50 |
3.7 nM
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Inhibition of cell viability against human MOLT-4 T-ALL cells incubated for 48 hrs by MTS assay.
Inhibition of cell viability against human MOLT-4 T-ALL cells incubated for 48 hrs by MTS assay.
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40239483 |
| MOLT-4 | DC50 |
0.43 nM
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Degradation of BCL-XL protein in human MOLT-4 T-ALL cells assessed via immunoblotting.
Degradation of BCL-XL protein in human MOLT-4 T-ALL cells assessed via immunoblotting.
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40239483 |
| Platelet | DC50 |
198 nM
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Degradation of BCL-XL protein in isolated human platelets assessed via immunoblotting.
Degradation of BCL-XL protein in isolated human platelets assessed via immunoblotting.
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40239483 |
In Vitro
XZ338 (compound 5e) potently inhibits the viability of MOLT-4 T-ALL cells with an IC50 of 3.7 nM, and binds to purified BCL-XL protein with a Ki value of 1.71 nM[1].
XZ338 exhibits 89-fold higher selectivity for MOLT-4 T-ALL cells than for isolated human platelets, and shows lower cytotoxicity against platelets relative to its anti-tumor activity[1].
XZ338 (0.1-1000 nM; 16 h) dose-dependently degrades BCL-XL protein in MOLT-4 T-ALL cells with a DC50 of 0.43 nM; it also degrades BCL-XL protein in isolated human platelets with a DC50 of 198 nM, which is significantly higher than that in MOLT-4 T-ALL cells[1].
XZ338 induces the formation of a ternary complex between BCL-XL and VHL proteins in vitro[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, human platelets
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Concentration:0, 0.1, 0.3, 1, 3, 10, 30, 100 nM (MOLT-4 T-ALL cells)
0, 0.1, 0.3, 1, 3, 10, 30, 100, 1000 nM (human platelets) -
Incubation Time:16 h
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Result:Demonstrated dose‑dependent reduction of BCL‑XL protein levels in MOLT‑4 cells, with a DC50 value of 0.43 nM.
Found that XZ338 degraded BCL‑XL only at high concentrations in human platelets, and obtained a DC50 value of 198 nM in human platelets
Observed that the DC50 value of XZ338 in human platelets was markedly higher than the DC50 value measured in MOLT‑4 cells.
Chemical Information
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Appearance Solid
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Peso molecular 1290.66
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Fòrmula C69H83N11O8S3
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Color Off-white to light yellow
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SMILES
O=C(NC1=NC2=CC=CC=C2S1)C3=CC=CC4=C3CN(C5=CC=C(C6=C(C)N(CC7(C[C@H]8C9)C[C@H]9C[C@H](C8)C7)N=C6)C(C(NS(CCCCCCCC(N[C@@H](C(C)(C)C)C(N%10[C@H](C(N[C@@H](C)C%11=CC=C(C%12=C(C)N=CS%12)C=C%11)=O)C[C@@H](O)C%10)=O)=O)(=O)=O)=O)=N5)CC4
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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 (77.48 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)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (1.94 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (1.94 mM); Suspended solution
This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (281 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 | 0.7748 mL | 3.8740 mL | 7.7480 mL | 19.3699 mL |
| 5 mM | 0.1550 mL | 0.7748 mL | 1.5496 mL | 3.8740 mL | |
| 10 mM | 0.0775 mL | 0.3874 mL | 0.7748 mL | 1.9370 mL | |
| 15 mM | 0.0517 mL | 0.2583 mL | 0.5165 mL | 1.2913 mL | |
| 20 mM | 0.0387 mL | 0.1937 mL | 0.3874 mL | 0.9685 mL | |
| 25 mM | 0.0310 mL | 0.1550 mL | 0.3099 mL | 0.7748 mL | |
| 30 mM | 0.0258 mL | 0.1291 mL | 0.2583 mL | 0.6457 mL | |
| 40 mM | 0.0194 mL | 0.0968 mL | 0.1937 mL | 0.4842 mL | |
| 50 mM | 0.0155 mL | 0.0775 mL | 0.1550 mL | 0.3874 mL | |
| 60 mM | 0.0129 mL | 0.0646 mL | 0.1291 mL | 0.3228 mL |
XZ338 Related Classifications
HY-172798 Related Classifications
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