GSK4418959
Based on 1 Customer Validation
GSK4418959 (IDE275) is a selective, reversible and orally active WRN helicase inhibitor. GSK4418959 shows >10,000-fold selectivity over other helicases. GSK4418959 inhibits ATPase and DNA unwinding functions in an ATP-competitive manner. GSK4418959 can be used for the study of microsatellite instability-high (MSI-H) cancer, such as colorectal cancer (CRC) and endometrial cancer (EC).
For research use only. We do not sell to patients.
- Purity: 99.07%
- CAS No.: 3064599-36-3
- Formula: C31H30F4N4O5S
- Molecular Weight:646.65
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Storage: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]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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Helicase |
GSK4418959 (0.1-100 µM; 5 days) selectively inhibits the proliferation of MSI-H cells, across different tumor types. Importantly, no response is observed in analogous microsatellite stable (MSS) cells[1].
GSK4418959 (0.001-100 µM) binds to WRN in HCT116 and HT29[1].
GSK4418959 (5 µM) downregulates WRN and upregulates GDF15 in cells. WRN downregulation occurs in both p53 wt (SW48) and mut MSI-H lines (LS411N) but GDF15 upregulation is only observed in SW48 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEC251 (MSS EC), HEC6 (MSI-H EC), SW48 (MSI-H CRC), and SW620 (MSS CRC) cells
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Concentration:0.1 µM, 1 µM, 10 µM, 100 µM
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Incubation Time:5 days
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Result:Selectively inhibited the proliferation of MSI-H cells, across different tumor types .
No response was observed in analogous microsatellite stable (MSS) cells.
GSK4418959 (30-300 mg/kg; oral; once daily; 3 days) shows dose-dependent induction of γH2AX, pKAP1, and p21 in SW48 xenograft tumors in a dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SW48 xenograft tumors[1]
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Dosage:10 mg/kg, 50 mg/kg, 100 mg/kg
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Administration:Oral; once daily; 24 days
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Result:Demonstrated dose-dependent antitutmor activity, including tumor regression in SW48 xenograt tumor models.
No response was observed in analogous microsatellite stable (MSS) models.
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Animal Model:SW48 xenograft tumors[1]
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Dosage:30 mg/kg, 100 mg/kg, or 300 mg/kg
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Administration:Oral; once daily; 3 days
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Result:Showed dose-dependent induction of γH2AX, pKAP1, and p21 in SW48 xenograft tumors in a dose-dependent manner.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 3064599-36-3
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Appearance Solid
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Molecular Weight 646.65
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Formula C31H30F4N4O5S
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Color White to off-white
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SMILES
O=C(NC1=CC=C(C(F)(F)F)C=C1F)[C@@H]2CCC[C@H](C3=CC=C(N(C)S(=O)(C4=CC(N=C(C)N5C)=C5C=C4)=O)C=C3)[C@H]2C(O)=O
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Synonyms
IDE275
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (154.64 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)
Purity & Documentation
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Data Sheet (275 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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. 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 | 1.5464 mL | 7.7322 mL | 15.4643 mL | 38.6608 mL |
| 5 mM | 0.3093 mL | 1.5464 mL | 3.0929 mL | 7.7322 mL | |
| 10 mM | 0.1546 mL | 0.7732 mL | 1.5464 mL | 3.8661 mL | |
| 15 mM | 0.1031 mL | 0.5155 mL | 1.0310 mL | 2.5774 mL | |
| 20 mM | 0.0773 mL | 0.3866 mL | 0.7732 mL | 1.9330 mL | |
| 25 mM | 0.0619 mL | 0.3093 mL | 0.6186 mL | 1.5464 mL | |
| 30 mM | 0.0515 mL | 0.2577 mL | 0.5155 mL | 1.2887 mL | |
| 40 mM | 0.0387 mL | 0.1933 mL | 0.3866 mL | 0.9665 mL | |
| 50 mM | 0.0309 mL | 0.1546 mL | 0.3093 mL | 0.7732 mL | |
| 60 mM | 0.0258 mL | 0.1289 mL | 0.2577 mL | 0.6443 mL | |
| 80 mM | 0.0193 mL | 0.0967 mL | 0.1933 mL | 0.4833 mL | |
| 100 mM | 0.0155 mL | 0.0773 mL | 0.1546 mL | 0.3866 mL |
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