Chemical Structure : SRX3177
CAS No.: 2241237-51-2
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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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.
M.Wt | 584.695 | |
Formula | C31H32N6O4S | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
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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 |
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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