2662512-15-2
Chemical Structure
Birelentinib
Synonym(s): DZD8586
- CAS No.: 2662512-15-2
- Formula:C23H21F2N5O3
- Molecular Weight:453.44
InChIKey: NQJKXHPWHYRGST-ZBFHGGJFSA-N
SMILES: NC1=NC=NN2C([C@@H]3CC[C@H](OC3)CO)=NC(C4=CC=C(C=C4)OC5=C(C(F)=CC=C5)F)=C12
Biological Activity: Birelentinib (DZD8586) is an orally effective, selective, non-covalent inhibitor targeting LYN tyrosine kinase and BTK tyrosine kinase, capable of penetrating the blood-brain barrier. Birelentinib exhibits concentration-dependent antiproliferative effects in RI-1 cells and diffuse large B-cell lymphoma (DLBCL) cell lines carrying BTK resistance mutations (such as C481X, V416L, etc.). Birelentinib blocks both BTK-dependent and independent signaling of the B-cell receptor (BCR), thereby inhibiting tumor cell proliferation and inducing cell death. Birelentinib can be used in research to overcome resistance to existing covalent and non-covalent BTK inhibitors in B-cell non-Hodgkin lymphoma (B-NHL)[1][2].
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Birelentinib | Birelentinib (DZD8586) is an orally effective, selective, non-covalent inhibitor targeting LYN tyrosine kinase and BTK tyrosine kinase, capable of penetrating the blood-brain barrier. Birelentinib exhibits concentration-dependent antiproliferative effects in RI-1 cells and diffuse large B-cell lymphoma (DLBCL) cell lines carrying BTK resistance mutations (such as C481X, V416L, etc.). Birelentinib blocks both BTK-dependent and independent signaling of the B-cell receptor (BCR), thereby inhibiting tumor cell proliferation and inducing cell death. Birelentinib can be used in research to overcome resistance to existing covalent and non-covalent BTK inhibitors in B-cell non-Hodgkin lymphoma (B-NHL). | |||||||||||||||||||||
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References
- [1]. Bai Y, et al. Preclinical Study of DZD8586, a Non-Covalent LYN/BTK Dual Inhibitor with Excellent BBB Penetration, for the Treatment of B-Cell Non-Hodgkin Lymphoma (B-NHL)[J]. Blood, 2023, 142: 2822.
- [2]. Song Y, et al. First report of phase 1 studies of DZD8586, a BBB penetrant LYN/BTK dual inhibitor, in patients with B-cell non-Hodgkin lymphoma (B-NHL)[J]. Blood, 2023, 142: 4465.
