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SRX3177

Chemical Structure : SRX3177

CAS No.: 2241237-51-2

SRX3177 (SRX 3177)

Catalog No.: PC-73383Not For Human Use, Lab Use Only.

SRX3177 is a potent, triple BRD4/PI3K/CDK4/6 inhibitor with nanomolar potency against PI3Kα (IC50=79 nM), BRD4 bromodomains (BD1 and BD2) (IC50=33 nM and 89 nM, respectively), and CDK4/6 (IC50=2.5/3.3 nM).

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Biological Activity

SRX3177 is a potent, triple BRD4/PI3K/CDK4/6 inhibitor with nanomolar potency against PI3Kα (IC50=79 nM), BRD4 bromodomains (BD1 and BD2) (IC50=33 nM and 89 nM, respectively), and CDK4/6 (IC50=2.5/3.3 nM).
SRX3177 is capable of targeting BRD4, PI3K and CDK4/6 simultaneously, induces apoptosis and cell cycle arrest and has in vitro efficacy in mantle cell lymphoma, hepatocellular carcinoma and neuroblastoma models.
SRX3177 has antitumor efficacy in in vivo xenograft models and is less toxic than the combination of agents that inhibit individual targets.

Physicochemical Properties

M.Wt 584.695
Formula C31H32N6O4S
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

7-Cyclopentyl-N,N-dimethyl-2-((4-(5-morpholino-7-oxo-7H-thieno[3,2-b]pyran-3-yl)phenyl)amino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide

References

1. Kendra R Vann, et al. Sci Rep. 2020 Jul 21;10(1):12027.

2. Adam M Burgoyne, et al. Cell Discov. 2020 Jul 28;6(1):49.

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