SRX3212
SRX3212 is a potent PI3Kα/BRD4 inhibitor with human IC50 values of 22 nM, 3.7 nM, and 32 nM for PI3Kα, BRD4BD1, and BRD4BD2, respectively. SRX3212 inhibits PI3K kinase activity and blocks acetyllysine binding function of BRD4BD1 and BRD4BD2. SRX3212 can be used for the research of mantle cell lymphoma, colon carcinoma, neuroblastoma, prostate cancer[1].
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- CAS. Nr.: 2735720-80-4
- Formel: C26H23N3O6S
- Molecular Weight:505.54
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
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Help & FAQs
Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
PI3Kα 22 nM (IC50) |
BD1 3.7 nM (IC50) |
BD2 32 nM (IC50) |
In Vitro
SRX3212 potently inhibits purified BRD4BD1 (IC50 = 3.7 nM) and BRD4BD2 (IC50 = 32 nM) in an AlphaScreen displacement binding assay[1].
SRX3212 potently inhibits purified PI3Kα with an IC50 of 22 nM in a fluorescence-based kinase screening assay[1].
SRX3212 binds tightly to the hydrophobic pocket of purified BRD4BD1 via multiple conserved and unique interactions, acting as an acetyllysine mimetic to drive high binding potency[1].
SRX3212 (48 hours) potently inhibits viability of JeKo-1 (IC50 = 0.28 μM), Mino (IC50 = 0.44 μM), and Z138 (IC50 = 0.24 μM) mantle cell lymphoma cell lines, HCT116 colon carcinoma cells (IC50 = 1.3 μM), and SKNBE-2 neuroblastoma cells (IC50 = 3.2 μM), but does not inhibit PC3 prostate cancer cell viability[1].
SRX3212 (0.5-5 μM; 1 hour) inhibits PI3K activity in JeKo-1 mantle cell lymphoma cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:JeKo-1 mantle cell lymphoma cell line
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Concentration:0.5 μM; 1 μM; 2.5 μM; 5 μM
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Incubation Time:1 hour
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Result:Caused a concomitant decrease in AKT phosphorylation at Ser473 with increasing concentrations, indicating reduced PI3K activity.
Chemical Information
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CAS. Nr. 2735720-80-4
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Molecular Weight 505.54
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Formel C26H23N3O6S
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SMILES
O=C1C=C(N2CCOCC2)OC3=C1SC=C3C4=CC(C(NCC5=CC=CN=C5)=O)=C6OCCOC6=C4
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
SRX3212 Related Classifications
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