KG-FP-003
KG-FP-003 is a highly potent, selective, and durable TEAD PROTAC degrader (TEAD1 DC50 = 6 ± 4 nM, TEAD2 DC50 = 68 ± 15 nM, TEAD3 DC50 = 12 ± 5 nM, TEAD4 DC50 = 7 ± 5 nM). KG-FP-003 promotes ubiquitination and degradation of TEAD. KG-FP-003 exhibits anticancer activity against mesothelioma and ovarian cancer.
(Pink: TEAD ligand (HY-186118); Blue: Cereblon E3 ligase ligand; Black: linker).
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- CAS No.: 3066008-42-9
- Formule: C58H67ClF2N6O8
- Masse moléculaire:1049.64
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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
- Pureté et documentation
- Références
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Activité biologique
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Cereblon |
TEAD1 6 nM (DC50) |
TEAD2 68 nM (DC50) |
TEAD3 12 nM (DC50) |
TEAD4 7 nM (DC50) |
KG-FP-003 binds to recombinant CRBN-DDB1ΔBPB protein with an IC50 of 591 ± 21 nM[1].
KG-FP-003 (3-fold serial dilution starting at 10 μM; 2 h) binds to CRBN in HEK293T cells overexpressing NanoLuc-CRBN, with an IC50 of 962 ± 86 nM in the cellular binding assay[1].
KG-FP-003 (6 h) potently and selectively degrades all four TEAD isoforms in HiBiT-tagged HEK293T cells after 6 h of treatment (TEAD1 DC50 = 6 ± 4 nM, TEAD2 DC50 = 68 ± 15 nM, TEAD3 DC50 = 12 ± 5 nM, TEAD4 DC50 = 7 ± 5 nM)[1].
KG-FP-003 (72 h potently inhibits the proliferation of NCI-H226 mesothelioma cells, with an IC50 of 27 ± 7 nM after 72 h of treatment[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MSTO-211H mesothelioma cells
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Concentration:300 nM
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Incubation Time:Unclear
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Result:Induced dramatic upregulation of the pro-apoptotic gene BMF and downregulation of the TEAD target gene CTGF.
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Cell Line:MSTO-211H mesothelioma cells
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Concentration:100-1000 nM
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Incubation Time:24 h
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Result:Increased the percentage of cells in G1 phase from 54.3% to 62.1% at 100 nM, and to 65.2% at 1000 nM, indicating G1 phase cell cycle arrest.
KG-FP-003 (10-30 mg/kg; i.p.; once daily; 21 days) induces significant tumor regression in ES2 ovarian carcinoma xenografts at doses of 10 mg/kg and 30 mg/kg[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (6-week-old)[1]
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Dosage:3 mg/kg; 10 mg/kg; 30 mg/kg
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Administration:i.p.; once daily; 21 days
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Result:Induced pronounced degradation of TEAD1 protein and significant tumor growth inhibition compared to vehicle controls.
Achieved a tumor growth inhibition (TGI) rate of 118% at 10 mg/kg.
Achieved a TGI rate of 129% at 30 mg/kg.
Maintained stable body weights in all treated mice throughout the 21-day treatment period.
Chemical Information
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CAS No. 3066008-42-9
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Masse moléculaire 1049.64
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Formule C58H67ClF2N6O8
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SMILES
CNC(C1=[C@](C(F)=C2C(C[C@@H]([C@@H]2O)C)=C1)[C@]3=C(C(F)=CC4=C3C[C@@](C5=CC=CC=C5)(O4)CNC6CCC(CC6)C(N7CCC(CC7)CC8CCN(CC8)C(COC9=CC=C(C(C)=C9)N%10CCC(NC%10=O)=O)=O)=O)Cl)=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)
KG-FP-003 Related Classifications
HY-186117 Related Classifications
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