GW296115
Based on 1 Customer Validation
GW296115 is a multi-target inhibitor with the following IC50 values against its targets: 8.4 nM for BRSK2, 21 nM for BRSK1, 1.8 μM for PDGFRβ, 5.5 nM for STK17B/DRAK2, 28 nM for DRAK1, 20 nM for PHKG1, and 89 nM for DCAMKL3. GW296115 downregulates the phosphorylation of S317 site on ULK1 and S351 site on P62, which are AMPK substrates driven by BRSK2. GW296115 does not alter the phosphorylation level of AMPK at T172, reduces nutrient deprivation-mediated Autophagy and autophagosome formation, and enhances Apoptosis. GW296115 exhibits anticancer activity against triple-negative breast cancer. GW296115 is applicable for breast cancer-related research.
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- Pureté: 98.68%
- CAS No.: 118458-58-5
- Formule: C22H15N3O4
- Masse moléculaire:385.37
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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PDGFRβ 1.8 μM (IC50) |
ULK1 |
DRAK1 28 nM (IC50) |
DRAK2 5.5 nM (IC50) |
GW296115 (1 μM) inhibits 25 out of 403 wild-type human kinases by over 90% at a concentration of 1 μM, with a selectivity index of 0.062[1].
GW296115 potently inhibits 6 IDG dark kinases in enzymatic assays, with IC50 values ranging from 5.5 nM (DRAK2) to 89 nM (DCAMKL3)[1].
GW296115 (1 μM; 72 h) exerts no effect on cell proliferation in 17 tested cancer cell lines and normal cell lines (including non-malignant MCF10A and MRC-5) following treatment at 1 μM for 72 h[1].
GW296115 (incubated for 2 h) potently binds to BRSK2 in living HEK293 cells with an IC50 of 107 nM, confirming that it is a cell-active BRSK2 inhibitor[1].
GW296115 (2.5 μM; 2-6 h) abolishes BRSK2-induced phosphorylation of AMPK substrates in HEK293T cells (this effect is observed at both 2 h and 6 h) and induces hyperphosphorylation of BRSK2 at the T174 site[1].
GW296115 (2-5 μM) inhibits autophagy and enhances apoptosis in MDA-MB-231 triple-negative breast cancer cells, while it also inhibits autophagy and enhances apoptosis in BT-474 estrogen receptor-positive breast cancer cells[2].
GW296115 (2 μM; 24 h) inhibits the growth of MDA-MB-231 triple-negative breast cancer cells[2].
GW296115 (2-3 μM; 72 h) reduces the 3D invasiveness of MDA-MB-231 triple-negative breast cancer cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:17 cancer and normal cell lines (including SUM159, MCF7, MCF10A, HCC1954, COV362, Kuramochi, PC-3, DU145, H729, HCT116, A549, MRC-5, Colo829, A375, Cas1, HPAF-II, Panc-1)
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Concentration:1 μM
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Incubation Time:72 h
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Result:Did not impact cell growth in any of the tested cell lines, and is considered generally non-toxic to cells.
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Cell Line:HEK293T cells transiently expressing hcRED, wild-type BRSK2, or kinase-dead BRSK2 (K48A, T174A)
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Concentration:2.5 μM
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Incubation Time:2 h, 6 h
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Result:Ablated wild-type BRSK2-induced AMPK substrate phosphorylation at both 2-h and 6-h time points.
Left phosphorylation of AMPK at T172 unaltered, but hyper-induced phosphorylation of BRSK2 at T174 in all samples except those expressing BRSK2 T174A.
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Cell Line:MDA-MB-231
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Concentration:2-3 μM
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Incubation Time:72 h
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Result:Reduced 3D Matrigel tumor cell invasiveness (invadopodia per spheroid) by over 75% compared to vehicle control.
Chemical Information
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CAS No. 118458-58-5
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Appearance Solid
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Masse moléculaire 385.37
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Formule C22H15N3O4
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Color Yellow to brown
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SMILES
O=C1NC(C2=C3C4=C(C=CC(OC)=C4)NC3=C5NC6=CC=C(OC)C=C6C5=C21)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvant et solubilité
DMSO : 50 mg/mL (129.75 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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)
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 (6.49 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 (6.49 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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
Pureté et documentation
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Fiche technique (282 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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Instruction de manipulation (2659 KB)
Références
[1]. Tamir TY, et al. PKIS deep dive yields a chemical starting point for dark kinases and a cell active BRSK2 inhibitor. Sci Rep. 2020 Sep 28;10(1):15826. [Content Brief]
[2]. Maiti A, et al. BRSK2 plays a role in autophagy and cancer cell growth and survival under nutrient deprivation stress via the PIK3C3 pathway. Sci Rep. 2025 Nov 19;15(1):40651. [Content Brief]
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 (sealed storage, away from moisture). 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 |
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| DMSO | 1 mM | 2.5949 mL | 12.9745 mL | 25.9491 mL | 64.8727 mL |
| 5 mM | 0.5190 mL | 2.5949 mL | 5.1898 mL | 12.9745 mL | |
| 10 mM | 0.2595 mL | 1.2975 mL | 2.5949 mL | 6.4873 mL | |
| 15 mM | 0.1730 mL | 0.8650 mL | 1.7299 mL | 4.3248 mL | |
| 20 mM | 0.1297 mL | 0.6487 mL | 1.2975 mL | 3.2436 mL | |
| 25 mM | 0.1038 mL | 0.5190 mL | 1.0380 mL | 2.5949 mL | |
| 30 mM | 0.0865 mL | 0.4325 mL | 0.8650 mL | 2.1624 mL | |
| 40 mM | 0.0649 mL | 0.3244 mL | 0.6487 mL | 1.6218 mL | |
| 50 mM | 0.0519 mL | 0.2595 mL | 0.5190 mL | 1.2975 mL | |
| 60 mM | 0.0432 mL | 0.2162 mL | 0.4325 mL | 1.0812 mL | |
| 80 mM | 0.0324 mL | 0.1622 mL | 0.3244 mL | 0.8109 mL | |
| 100 mM | 0.0259 mL | 0.1297 mL | 0.2595 mL | 0.6487 mL |
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