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).
Para uso exclusivo en investigación. No vendemos a pacientes.
- No. CAS: 3066008-42-9
- Fòrmula: C58H67ClF2N6O8
- Peso molecular:1049.64
-
Almacenamiento:
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]
-
Actividad biológica
-
Chemical Information
- Pureza y Documentación
- Referencias
-
Help & FAQs
Ver todos los productos específicos de isoformas YAP
MoreVer todos los productos específicos de isoformas PROTACs
More
Actividad biológica
Descripciòn
IC50 & Target
[1]|
Cereblon |
TEAD1 6 nM (DC50) |
TEAD2 68 nM (DC50) |
TEAD3 12 nM (DC50) |
TEAD4 7 nM (DC50) |
In Vitro
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.
-
Cell Line:MSTO-211H mesothelioma cells
-
Concentration:300 nM
-
Incubation Time:Unclear
-
Result:Induced dramatic upregulation of the pro-apoptotic gene BMF and downregulation of the TEAD target gene CTGF.
-
Cell Line:MSTO-211H mesothelioma cells
-
Concentration:100-1000 nM
-
Incubation Time:24 h
-
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.
Parmacokinetics
In Vivo
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.
-
Animal Model:BALB/c nude (6-week-old)[1]
-
Dosage:3 mg/kg; 10 mg/kg; 30 mg/kg
-
Administration:i.p.; once daily; 21 days
-
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
-
No. CAS 3066008-42-9
-
Peso molecular 1049.64
-
Fòrmula C58H67ClF2N6O8
-
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
-
Envío
Room temperature in continental US; may vary elsewhere.
-
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)
KG-FP-003 Related Classifications
HY-186117 Related Classifications
Powered by Bioz