SRX3262 | BTK/PI3K/BRD4 inhibitor | Probechem Biochemicals

Chemical Structure : SRX3262

SRX3262 (SRX 3262, SRX-3262 )

Catalog No.: PC-73384Not For Human Use, Lab Use Only.

SRX3262 (SRX 3262, SRX 3262) is a potent, triple action BTK, PI3K and BRD4 inhibitor with potency against BTK (IC50=35 nM), PI3Kδ (IC50=16 nM), PI3Kα (IC50=64 nM), and both bromodomains of BRD4 (IC50 BD1=228 nM, IC50 BD2=348 nM).

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Biological Activity

SRX3262 (SRX 3262) is a potent, triple action BTK, PI3K and BRD4 inhibitor with potency against BTK (IC50=35 nM), PI3Kδ (IC50=16 nM), PI3Kα (IC50=64 nM), and both bromodomains of BRD4 (IC50 BD1=228 nM, IC50 BD2=348 nM).

SRX3262 shows dose-dependent antiproliferative activity in MCL cell lines with IC50 of 0.62 μM, 0.13 μM, and 1.2 μM for JeKo-1, Mino, and Ibrutinib-resistant Granta cells, respectively.

SRX3262 simultaneously blocks three interrelated MCL driver pathways: BTK, PI3K-AKT-mTOR and MYC.

SRX3262 concomitantly binds to BTK, PI3K, and BRD4, exhibits potent in vitro and in vivo activity against MCL, and overcomes the Ibrutinib resistance resulting from the BTK-C481S mutation.

SRX3262 inhibits IgM-induced BTK and AKT phosphorylation and abrogates binding of BRD4 to MYC loci.

SRX3262 promotes c-MYC destabilization, induces cell cycle arrest and apoptosis, and shows antitumor activity in in vivo xenograft models.

Physicochemical Properties

M.Wt	424.47
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-(4-acryloyl-3,4-dihydro-2H-benzo[b][1,4]oxazin-6-yl)-5-morpholino-7H-thieno[3,2-b]pyran-7-one

References

1. Dhananjaya Pal, et al. iScience. 2021 Jul 30;24(9):102931.

SRX3262 (SRX 3262, SRX-3262 )

Biological Activity

Physicochemical Properties

References

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