WRN-IN-24
WRN-IN-24 is an orally active allosteric covalent Werner syndrome helicase (WRN) inhibitor with an IC50 of 201 nM. WRN-IN-24 binds to a novel allosteric cavity, forms an additional hydrogen bond with K894, and functionally inhibits WRN activity. WRN-IN-24 inhibits colorectal cancer cells proliferation and exerts dose-dependent antitumor activity in xenograft mouse models. WRN-IN-24 can be used for the research of microsatellite instability-high cancers, including colorectal cancer.
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- CAS No.: 3113010-46-8
- Formule: C24H28F3N5O6S2
- Masse moléculaire:603.63
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
[1]|
Helicase |
In Vitro
WRN-IN-24 (Compound 22) potently inhibits purified WRN helicase activity with an IC50 of 201 nM[1].
WRN-IN-24 potently inhibits the proliferation of HCT116 MSI-H colorectal cancer cells with an IC50 of 49 nM[1].
WRN-IN-24 activates the DNA damage response marker γH2AX in SW48 MSI-H colorectal cancer cells with an EC50 of 338 nM[1].
WRN-IN-24 potently inhibits the proliferation of SW48 MSI-H colorectal cancer cells with an IC50 of 48.0 nM[1].
WRN-IN-24 shows no proliferation inhibitory activity against HT29 and MDA-MB-231 MSS cell lines, with IC50 values > 10000 nM for both[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | CL | Vdss | T1/2 | Cmax | AUC0-last | F |
|---|---|---|---|---|---|---|---|---|
| Mice[1] | 1 mg/kg | i.v. | 0.82 L/h/kg | 3.36 L/kg | 3.20 h | / | / | / |
| Mice[1] | 10 mg/kg | p.o. | / | / | / | 1393 ng/mL | 10152 ng·h/mL | 98.1 % |
| Rat[1] | 1 mg/kg | i.v. | 0.70 L/h/kg | 2.63 L/kg | 4.42 h | / | / | / |
| Rat[1] | 10 mg/kg | p.o. | / | / | / | 782 ng/mL | 7751 ng·h/mL | 55.5 % |
| Dog[1] | 1 mg/kg | i.v. | 0.11 L/h/kg | 4.37 L/kg | 28.8 h | / | / | / |
| Dog[1] | 5 mg/kg | p.o. | / | / | / | 869 ng/mL | 14960 ng·h/mL | 71.5 % |
| Monkey[1] | 1 mg/kg | i.v. | 0.20 L/h/kg | 1.54 L/kg | 5.89 h | / | / | / |
| Monkey[1] | 5 mg/kg | p.o. | / | / | / | 1267 ng/mL | 19069 ng·h/mL | 82.6 % |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mice HCT116 (MSI-H) xenograft[1]
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Dosage:5, 10 and 20 mg/kg
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Administration:P.o.; daily for 21 days
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Result:Inhibited tumor growth with TGI of 95.2% at 20 mg/kg.
Chemical Information
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CAS No. 3113010-46-8
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Masse moléculaire 603.63
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Formule C24H28F3N5O6S2
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SMILES
O=C(C1=C(OC2=CC=CC=C2)N=C(C(F)(F)C)N=C1NC3CN(S(=O)(C)=O)C3)N[C@@H](C4CC4)/C=C(F)/S(=O)(C)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
WRN-IN-24 Related Classifications
HY-181562 Related Classifications
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Keywords
- WRN-IN-24
- 3113010-46-8
- DNA/RNA Synthesis
- SW48 MSI-H colorectal cancer cells
- K894
- colorectal cancer
- HT29 MSS cell lines
- HCT116 MSI-H colorectal cancer cells
- microsatellite instability-high cancers
- MDA-MB-231 MSS cell lines
- xenograft mouse models
- colorectal cancer cells
- Werner syndrome helicase
- Inhibitor
- inhibitor
- inhibit