ZLY025
Based on 1 Customer Validation
ZLY025 is a potent and orally active CCNK molecular glue degrader with an DC50 of 42.7 nM. ZLY025 exhibits broad-spectrum antiproliferative activity against various tumor cells with IC50 values ranging from 0.08 to 2.45 μM. ZLY025 can induce cells apoptosis and G1 phase arrest. ZLY025 can be used for the research of cancer, such as lung cancer.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 99.40%
- CAS No.: 3070379-34-6
- 화학식: C15H13N3O2S
- 분자량:299.35
-
보관:Powder -20°C, 3 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]
-
Biological Activity
-
Chemical Information
-
용액&용해도
- 순도&문서
- References
-
Help & FAQs
Biological Activity
제품 설명
In Vitro
ZLY025 exhibits broad-spectrum antiproliferative activity against various tumor cell lines including lung cancer, breast cancer, liver cancer, and leukemia, with IC50 values ranging from 0.08 to 2.45 μM[1].
ZLY025 (125-500 nM; 24 h) induces A549 cells apoptosis and G1 phase arrest[1].
ZLY025 (30-1000 nM; 8-24 h) reduces expression of CCNK, CDK12, p-CTD, and BRCA1 in A549 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:A549 cells
-
Concentration:125, 250, 500 nM
-
Incubation Time:24 h
-
Result:Increased apoptosis rate.
-
Cell Line:A549 cells
-
Concentration:125, 250, 500 nM
-
Incubation Time:24 h
-
Result:Induced G1 phase arrest.
-
Cell Line:A549 cells
-
Concentration:30, 100, 300, 1000 nM
-
Incubation Time:8, 16, 24 h
-
Result:Decreased expression of CCNK, CDK12, p-CTD, and BRCA1.
Parmacokinetics
| Species | Dose | Route | Note | Tmax | Cmax | T1/2 | AUC0-t | CL |
|---|---|---|---|---|---|---|---|---|
| Rat | 3 mg/kg | p.o. | 文献审核 | 0.6 h | 180.18 ng/mL | 6.82 h | 1184.94 ng·h/mL | 2.6 L/h/kg |
In Vivo
ZLY025 (200 mg/kg, i.g., once daily for 14 days) shows extremely low subacute toxicity in ICR mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:BALB/c nude (female, subcutaneous injection of A549 human non-small cell lung cancer (NSCLC) cells)[1]
-
Dosage:10, 20, 40 mg/kg
-
Administration:Oral gavage; once daily for 17 days
-
Result:Reduced tumor weight and volume.
Did not affect mouse body weight or cause toxicity to major organs.
Chemical Information
-
CAS No. 3070379-34-6
-
Appearance Solid
-
분자량 299.35
-
화학식 C15H13N3O2S
-
Color White to off-white
-
SMILES
CC1=CN=C(NC(CC2=CC=C(C=C2)C3=NC=CO3)=O)S1
-
선적
Room temperature in continental US; may vary elsewhere.
-
보관
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
In Vitro:
DMSO : 5 mg/mL (16.70 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: ≥ 0.5 mg/mL (1.67 mM); Clear solution
This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%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.
순도&문서
-
Data Sheet (274 KB)
-
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
-
Handling Instructions (2659 KB)
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 | 3.3406 mL | 16.7029 mL | 33.4057 mL | 83.5143 mL |
| 5 mM | 0.6681 mL | 3.3406 mL | 6.6811 mL | 16.7029 mL | |
| 10 mM | 0.3341 mL | 1.6703 mL | 3.3406 mL | 8.3514 mL | |
| 15 mM | 0.2227 mL | 1.1135 mL | 2.2270 mL | 5.5676 mL |
ZLY025 Related Classifications
HY-179289 Related Classifications
Powered by Bioz