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Chemical Structure : SRX3305
Catalog No.: PC-73385Not For Human Use, Lab Use Only.
SRX3305 is a potent, triple BTK/PI3K/BRD4 inhibitor with IC50 of 6.5 nM, 15 nM, and 4 nM toward BTK, PI3Kɑ and PI3Kδ respectively, inhibits BRD4 BD1 and BD2 with IC50 of 77 and 95 nM.
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SRX3305 is a potent, triple BTK/PI3K/BRD4 inhibitor with IC50 of 6.5 nM, 15 nM, and 4 nM toward BTK, PI3Kα and PI3Kδ respectively, inhibits BRD4 BD1 and BD2 with IC50 of 77 and 95 nM.
SRX3305 showed enhanced binding to the drug-resistant C481S mutant of BTK compared to SRX3262 (IC50=9 uM and 25 uM, respectively).
SRX3305 displayed cytotoxicity aginst MCL cell lines JeKo-1, Mino, Granta with IC50 of 58 nM, 1 nM, 1.1 uM, respectively.
SRX3305 inhibited cell vbiability of JeKo-1 BTK C481S and Mino BTK C481S mutant cell lines with IC50 of 1 uM and 47 nM, respectively, with minimally toxic to healthy donor PBMCs.
SRX3305 showed improved efficacy in MCL and Ibrutinib-resistant MCL cells, SRX3305 impacted gene expression, perturbs the cell cycle and promotes apoptosis in MCL.
| M.Wt | 424.471 | |
| Formula | C22H20N2O5S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Kendra R Vann, et al. Mol Biomed. 2022 Jan 15;3(1):2.
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