KWR137
KWR137 is an orally active Werner protein (WRN) inhibitor with a human IC50 of 8 nM. KWR137 inhibits the ATPase activity required for WRN helicase function, induces WRN protein degradation, suppresses cancer cell proliferation, and slows tumor growth without causing weight loss or off-target effects. KWR137 can be used for the research of colorectal cancer.
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- Fòrmula: C33H31ClF3N9O4
- Peso molecular:710.11
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
WRN 8 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| SW48 | GI50 |
0.509 μM
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Antiproliferative activity against human MSI-H colorectal cancer SW48 cells assessed after 3 or 4 days of treatment.
Antiproliferative activity against human MSI-H colorectal cancer SW48 cells assessed after 3 or 4 days of treatment.
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39956276 |
| HCT-116 | GI50 |
0.824 μM
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Antiproliferative activity against human MSI-H colorectal cancer HCT116 cells assessed after 3 or 4 days of treatment.
Antiproliferative activity against human MSI-H colorectal cancer HCT116 cells assessed after 3 or 4 days of treatment.
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39956276 |
| SW-620 | GI50 |
>20 μM
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Antiproliferative activity against human MSS colorectal cancer SW620 cells assessed after 3 or 4 days of treatment, with measured GI50 greater than 20 μM.
Antiproliferative activity against human MSS colorectal cancer SW620 cells assessed after 3 or 4 days of treatment, with measured GI50 greater than 20 μM.
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39956276 |
In Vitro
KWR137 (compound 10i) (3-4 days) inhibits proliferation of MSI-H colorectal cancer cell lines SW48 (GI50 = 0.509 μM) and HCT116 (GI50 = 0.824 μM), but has minimal activity against MSS colorectal cancer cell line SW620 (GI50 > 20 μM)[1].
KWR137 potently inhibits the ATPase activity of purified full-length human WRN protein with an IC50 of 8 nM[1].
KWR137 (10 μM; 18 h) induces WRN protein degradation in MSI-H colorectal cancer cell lines SW48 and HCT116, but not in MSS colorectal cancer cell line SW620[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MSI-H colorectal cancer cell lines SW48, HCT116; MSS colorectal cancer cell line SW620
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Concentration:10 μM
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Incubation Time:18 h
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Result:Induced degradation of WRN protein in SW48 and HCT116 (MSI-H) cells.
Did not cause WRN degradation in SW620 (MSS) cells.
Parmacokinetics
| Species | Dose | Route | Tmax | Cmax | T1/2 | AUClast | MRTlast |
|---|---|---|---|---|---|---|---|
| Mice[1] | 10 mg/kg | p.o. | 1.0 h | 0.6 μg/mL | 1.99 h | 2.61 μg·h/mL | 2.94 h |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD/SCID mice[1]
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Dosage:40 mg/kg
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Administration:p.o.; once daily; 14 days
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Result:Achieved a tumor growth inhibition rate of 49.3%.
Reduced tumor weight compared to vehicle control.
Caused no body weight loss or off-target effects.
Chemical Information
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Peso molecular 710.11
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Fòrmula C33H31ClF3N9O4
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SMILES
ClC1=CC(C(F)(F)F)=CC=C1NC(CN2C(CC)=C(N3CCN(C(C(N4)=CC5=C4C=CC=N5)=O)CC3)C(N6C2=NC(C7=CCOCC7)=N6)=O)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
KWR137 Related Classifications
HY-168934 Related Classifications
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