VRX0466617
Based on 1 Customer Validation
VRX0466617 is a selective and ATP-competitive Chk2 inhibitor with an IC50 of 120 nM and a Ki of 11 nM. VRX0466617 does not inhibit the related Chk1 activity. VRX0466617 can be used in the study of cancer.
For research use only. We do not sell to patients.
- Purity : 99.91%
- CAS No.: 926906-64-1
- Formula: C19H20BrN5O2S
- Molecular Weight:462.36
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Storage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
[1]|
Chk1 120 nM (IC50) |
Chk1 11 nM (Ki) |
In Vitro
VRX0466617 (10-30 μM) inhibits both the autophosphorylation of Chk2 and the phosphorylation of Cdc25C substrate in vitro kinase reactions[1].
VRX0466617 (0.05-10 μM; 30-180 min) inhibits the phosphorylation of Chk2 Ser19 and Ser33-35, but not of Chk2 Thr68 in ionizing radiation (IR)-induced cells[1].
VRX0466617 induces the phosphorylation of Chk2 Thr68 in the absence of DNA damage[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:LCL-N cells treated with ionizing radiation (IR).
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Concentration:0.05 μM, 0.5 μM, 5 μM, 10 μM
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Incubation Time:30 min, 180 min
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Result:Markedly inhibited the phosphorylation of Ser33-35 and, to a less extent, of Ser19, but not of Thr68.
Chemical Information
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CAS No. 926906-64-1
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Appearance Solid
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Molecular Weight 462.36
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Formula C19H20BrN5O2S
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Color White to off-white
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SMILES
OCC(C)NC(C(C(NS1)=O)=C1NC2=CC=C(NC3=CC=C(Br)C=C3)C=C2)=N
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvent & Solubility
In Vitro:
DMSO : ≥ 100 mg/mL (216.28 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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 and light). 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 and light). 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)
Protocols
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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.
Purity & Documentation
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Data Sheet (270 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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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 (sealed storage, away from moisture and light). 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 | 2.1628 mL | 10.8141 mL | 21.6282 mL | 54.0704 mL |
| 5 mM | 0.4326 mL | 2.1628 mL | 4.3256 mL | 10.8141 mL | |
| 10 mM | 0.2163 mL | 1.0814 mL | 2.1628 mL | 5.4070 mL | |
| 15 mM | 0.1442 mL | 0.7209 mL | 1.4419 mL | 3.6047 mL | |
| 20 mM | 0.1081 mL | 0.5407 mL | 1.0814 mL | 2.7035 mL | |
| 25 mM | 0.0865 mL | 0.4326 mL | 0.8651 mL | 2.1628 mL | |
| 30 mM | 0.0721 mL | 0.3605 mL | 0.7209 mL | 1.8023 mL | |
| 40 mM | 0.0541 mL | 0.2704 mL | 0.5407 mL | 1.3518 mL | |
| 50 mM | 0.0433 mL | 0.2163 mL | 0.4326 mL | 1.0814 mL | |
| 60 mM | 0.0360 mL | 0.1802 mL | 0.3605 mL | 0.9012 mL | |
| 80 mM | 0.0270 mL | 0.1352 mL | 0.2704 mL | 0.6759 mL | |
| 100 mM | 0.0216 mL | 0.1081 mL | 0.2163 mL | 0.5407 mL |
VRX0466617 Related Classifications
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