Chemical Structure : KG-FP-003
CAS No.:
3066008-42-9
KG-FP-003
Catalog No.: PC-25828Not For Human Use, Lab Use Only.
KG-FP-003 is a potent, selective, and durable TEAD PROTAC degrader with biochemicals binding IC50 of 591 nM for CRBN, degrades all TEAD isoforms in NCI-H1299 cells (TEAD1, DC50= 6 nM, TEAD2 DC50= 68 nM, TEAD3 DC50 =12, TEAD4 DC50= 7 nM).
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
KG-FP-003 is a potent, selective, and durable TEAD PROTAC degrader with biochemicals binding IC50 of 591 nM for CRBN, degrades all TEAD isoforms in NCI-H1299 cells (TEAD1, DC50= 6 nM, TEAD2 DC50= 68 nM, TEAD3 DC50 =12, TEAD4 DC50= 7 nM).
KG-FP-003 robustly induces formation of the TEAD1–CRBN ternary complex with EC50 of 8 nM.
KG-FP-003 markedly increases TEAD1 ubiquitination, promotes UPS-dependent degradation of TEAD1.
KG-FP-003 exhibits potent antiproliferative activity with IC50 values of 27 nM in NCI-H226 cells and 47 nM in MSTO-211H cells.
KG-FP-003 (3 mg/kg, i.p.) induces pronounced degradation of TEAD1 protein and significant tumor growth inhibition in MSTO-211H pleural mesothelioma xenograft model.
Physicochemical Properties
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M.Wt
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1049.65
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Formula
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C58H67ClF2N6O8
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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(1S,2S)-6-((2S)-5-chloro-2-((((1r,4S)-4-(4-((1-(2-(4-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-3-methylphenoxy)acetyl)piperidin-4-yl)methyl)piperidine-1-carbonyl)cyclohexyl)amino)methyl)-6-fluoro-2-phenyl-2,3-dihydrobenzofuran-4-yl)-7-fluoro-1-hydroxy-N,2-dimethyl-2,3-dihydro-1H-indene-5-carboxamide
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References
1. Cao L, et al. Adv Sci (Weinh). 2025 Oct 5:e03277.
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