SKLB-197
Based on 1 Customer Validation
SKLB-197 showed an IC50 value of 0.013 μM against ATR but very weak or no activity against other 402 protein kinases. It displayed potent antitumor activity against ATM-deficent tumors both in vitro and in vivo.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté : 99.91%
- CAS No.: 2713577-16-1
- Formule: C25H24N6O
- Masse moléculaire:424.50
-
Stockage: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]
-
Activité biologique
-
Chemical Information
-
Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
-
Help & FAQs
-
HY-15520
CGK733ATM/ATR Inhibitor -
HY-101566
ElimusertibATR Inhibitor -
HY-112305
AZ32ATM/ATR Inhibitor -
HY-139609
CamonsertibATR Inhibitor -
HY-109566
ElrelesertibATM Kinase Inhibitor -
HY-19959
MirinMre11-Rad50-Nbs1 Complex Inhibitor -
HY-12016
KU-55933ATM Inhibitor -
HY-13902
BerzosertibATR Inhibitor -
HY-19323
CeralasertibATR Inhibitor -
HY-14731
VE-821ATR Inhibitor -
HY-112198
AZ31ATM Inhibitor -
HY-11002
CP-466722ATM/ATR Inhibitor
Activité biologique
Description
IC50 & Target
|
ATR 0.013 μM (IC50) |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HT-29 | IC50 |
0.439 μM
Compound: 5m, SKLB-197
|
Antiproliferative activity against human HT-29 cells assessed as reduction in cell viability incubated for 72 hrs in presence of AZD1390 by MTT assay
Antiproliferative activity against human HT-29 cells assessed as reduction in cell viability incubated for 72 hrs in presence of AZD1390 by MTT assay
|
[PMID: 35183872] |
Chemical Information
-
CAS No. 2713577-16-1
-
Appearance Solid
-
Masse moléculaire 424.50
-
Formule C25H24N6O
-
Color White to light yellow
-
SMILES
CN1N=CC=C1C2=CC3=C(N4[C@H](C)COCC4)N=C(C5=CC=CC6=C5C=CN6)N=C3C=C2
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (235.57 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 (5.89 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.
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.
Protocole
-
Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
-
Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
Pureté et documentation
-
Fiche technique (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)
-
Instruction de manipulation (2659 KB)
Références
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 | 2.3557 mL | 11.7786 mL | 23.5571 mL | 58.8928 mL |
| 5 mM | 0.4711 mL | 2.3557 mL | 4.7114 mL | 11.7786 mL | |
| 10 mM | 0.2356 mL | 1.1779 mL | 2.3557 mL | 5.8893 mL | |
| 15 mM | 0.1570 mL | 0.7852 mL | 1.5705 mL | 3.9262 mL | |
| 20 mM | 0.1178 mL | 0.5889 mL | 1.1779 mL | 2.9446 mL | |
| 25 mM | 0.0942 mL | 0.4711 mL | 0.9423 mL | 2.3557 mL | |
| 30 mM | 0.0785 mL | 0.3926 mL | 0.7852 mL | 1.9631 mL | |
| 40 mM | 0.0589 mL | 0.2945 mL | 0.5889 mL | 1.4723 mL | |
| 50 mM | 0.0471 mL | 0.2356 mL | 0.4711 mL | 1.1779 mL | |
| 60 mM | 0.0393 mL | 0.1963 mL | 0.3926 mL | 0.9815 mL | |
| 80 mM | 0.0294 mL | 0.1472 mL | 0.2945 mL | 0.7362 mL | |
| 100 mM | 0.0236 mL | 0.1178 mL | 0.2356 mL | 0.5889 mL |
SKLB-197 Related Classifications
HY-144217 Related Classifications
Powered by Bioz