2941611-57-8
Chemical Structure
CFON-026
- CAS No.: 2941611-57-8
- Formula:C33H34N8O2
- Molecular Weight:574.68
InChIKey: MSKNOSLTYZTISS-ZOTOWQMDSA-N
SMILES: NC1=NC=C2/C=C/CCCCCC(N[C@@H]3CCC[C@@H](C4=NC(C5=CC=C(C(NC6=CC(C#N)=CC=N6)=O)C=C5)=C1N24)C3)=O
Biological Activity: CFON-026 is a selective, orally active and non-covalent BTK inhibitor with an IC50 of 0.27 nM. CFON-026 has significant antitumor activity against wild-type BTK (TMD8 and REC-1) and all clinically relevant BTK resistance mutations (BTK C481S, T474I, L528W and V416L). CFON-026 induces complete tumor regression in TMD8 xenograft mice model. CFON-026 can be used for research of hematological cancers like chronic lymphocytic leukemia and waldenström macroglobulinemia[1][2].
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CFON-026 | CFON-026 is a selective, orally active and non-covalent BTK inhibitor with an IC50 of 0.27 nM. CFON-026 has significant antitumor activity against wild-type BTK (TMD8 and REC-1) and all clinically relevant BTK resistance mutations (BTK C481S, T474I, L528W and V416L). CFON-026 induces complete tumor regression in TMD8 xenograft mice model. CFON-026 can be used for research of hematological cancers like chronic lymphocytic leukemia and waldenström macroglobulinemia. | |||||||||||||||||||||
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- [1]. de Man J, et al. CFON-026 is a potent non-covalent BTK inhibitor suitable for combination therapy with covalent BTK inhibitors for early eradication of resistance mutations. Cancer Research. 2024 Mar 22;84(6_Supplement):1960-.
- [2]. de Man J, et al. CFON-026 is a macrocycle that disrupts the BTK protein scaffold thereby inhibiting all clinically relevant BTK resistance mutations. Cancer Research. 2025 Apr 21;85(8_Supplement_1):3785-.
Keywords
