2409965-28-0
Chemical Structure
SRX3305
- CAS No.: 2409965-28-0
- Formula:C22H20N2O5S
- Molecular Weight:424.47
InChIKey: MDJZBGKTJDDFOO-UHFFFAOYSA-N
SMILES: O=C1C=C(N2CCOCC2)OC3=C1SC=C3C4=CC5=C(OCCN5C(C=C)=O)C=C4
Biological Activity: SRX3305 is an BTK/PI3K/BRD4 inhibitor with IC50s of 6.5 nM, 15 nM, and 4 nM toward BTK, PI3Kɑ and PI3Kδ, respectively. SRX3305 attenuates chronic lymphocytic leukemia (CLL) and mantle cell lymphoma (MCL) cell proliferation and promotes apoptosis in a dose-dependent fashion. SRX3305 yields potent anti-tumor effects but spares healthy bystander cells. SRX3305 inhibits the activation-induced proliferation of primary CLL cells in vitro and effectively blocks microenvironment-mediated survival signals. SRX3305 blocks CLL cell migration toward CXCL-12 and CXCL-13. SRX3305 maintains its anti-tumor effects in Ibrutinib (HY-10997)-resistant CLL cells. SRX3305 can be used for research in CLL, diffuse large B-cell lymphoma (DLBCL) and MCL[1][2].
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SRX3305 | SRX3305 is an BTK/PI3K/BRD4 inhibitor with IC50s of 6.5 nM, 15 nM, and 4 nM toward BTK, PI3Kɑ and PI3Kδ, respectively. SRX3305 attenuates chronic lymphocytic leukemia (CLL) and mantle cell lymphoma (MCL) cell proliferation and promotes apoptosis in a dose-dependent fashion. SRX3305 yields potent anti-tumor effects but spares healthy bystander cells. SRX3305 inhibits the activation-induced proliferation of primary CLL cells in vitro and effectively blocks microenvironment-mediated survival signals. SRX3305 blocks CLL cell migration toward CXCL-12 and CXCL-13. SRX3305 maintains its anti-tumor effects in Ibrutinib (HY-10997)-resistant CLL cells. SRX3305 can be used for research in CLL, diffuse large B-cell lymphoma (DLBCL) and MCL. | |||||||||||||||||||||
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- [1]. Smith AL, et al. A Novel Triple-Action Inhibitor Targeting B-Cell Receptor Signaling and BRD4 Demonstrates Preclinical Activity in Chronic Lymphocytic Leukemia. Int J Mol Sci. 2022 Jun 16;23(12):6712. [Content Brief]
- [2]. Vann KR, et al. Combinatorial inhibition of BTK, PI3K-AKT and BRD4-MYC as a strategy for treatment of mantle cell lymphoma. Mol Biomed. 2022 Jan 15;3(1):2. [Content Brief]
Keywords
