3005272-36-3
Chemical Structure
BMS-986458
- CAS No.: 3005272-36-3
- Formula:C32H34ClN9O3
- Molecular Weight:628.12
InChIKey: JALIPZPFONOAJA-ZKGBLMBJSA-N
SMILES: C[C@@H]1CN(CC[C@H]1NC2=CC=C3C(N(N=C3C4CCC(NC4=O)=O)C)=C2)C5=NC=C(C(NC6=CC7=C(N(C(C7)=O)C)C=C6)=N5)Cl
Biological Activity: BMS-986458 is a highly selective, orally active cereblon-based BCL6 PROTAC degrader and antitumor agent. BMS-986458 selectively degrades BCL6 by binding cereblon to the BTB domain of BCL6, thereby regulating the cell cycle, antiproliferative and interferon signaling pathways, and upregulating the expression and distribution of CD20. BMS-986458 modulates the phenotype of follicular helper T cells and reduces circulating tumor DNA levels. The combination of BMS-986458 with CD20xCD3 bispecific antibody also enhances the efficiency of T cell tumor infiltration and expansion. BMS-986458 induces regression of BCL6-positive tumors and prolongs survival, and it is suitable for research related to B-cell non-Hodgkin lymphoma, diffuse large B-cell lymphoma, follicular lymphoma, and relapsed/refractory lymphoma[1][2][3].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
|
|
BMS-986458 | 99.65% | BMS-986458 is a highly selective, orally active cereblon-based BCL6 PROTAC degrader and antitumor agent. BMS-986458 selectively degrades BCL6 by binding cereblon to the BTB domain of BCL6, thereby regulating the cell cycle, antiproliferative and interferon signaling pathways, and upregulating the expression and distribution of CD20. BMS-986458 modulates the phenotype of follicular helper T cells and reduces circulating tumor DNA levels. The combination of BMS-986458 with CD20xCD3 bispecific antibody also enhances the efficiency of T cell tumor infiltration and expansion. BMS-986458 induces regression of BCL6-positive tumors and prolongs survival, and it is suitable for research related to B-cell non-Hodgkin lymphoma, diffuse large B-cell lymphoma, follicular lymphoma, and relapsed/refractory lymphoma. | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
- [1]. Groocock L, et al. BMS-986458 a potential first-in-class, highly selective, potent and well tolerated BCL6 ligand directed degrader (LDD) demonstrates multi-modal anti-tumor efficacy for the treatment of B-cell non-Hodgkin's lymphoma[J]. Blood, 2024, 144: 957.
- [2]. Morschhauser F, et al. BMS-986458, a first-in-class, bifunctional cereblon-dependent ligand-directed degrader of B-cell lymphoma 6 (BCL6) in patients with Relapsed/Refractory (R/R) non-Hodgkin lymphoma (NHL): Updated results from the Phase 1 dose escalation study[J]. 2025.
- [3]. Deb G, et al. BMS-986458, a first-in-class, highly selective, and potent ligand-directed degrader (LDD) of B-cell lymphoma 6 (BCL6) combined with T-cell engagers (TCEs) demonstrates preclinical synergistic antitumor efficacy for the treatment of B-cell non-Hodgkin lymphoma (NHL)[J]. Blood, 2025, 146: 5090.
Keywords
