SRX3305 | BTK/PI3K/BRD4 inhibitor | Probechem Biochemicals

Chemical Structure : SRX3305

SRX3305 (SRX 3305)

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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Biological Activity

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.

Physicochemical Properties

M.Wt	424.471
Formula	C22H20N2O5S
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	3-[3,4-Dihydro-4-(1-oxo-2-propen-1-yl)-2H-1,4-benzoxazin-6-yl]-5-(4-morpholinyl)-7H-thieno[3,2-b]pyran-7-one

References

1. Kendra R Vann, et al. Mol Biomed. 2022 Jan 15;3(1):2.

SRX3305 (SRX 3305)

Biological Activity

Physicochemical Properties

References

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