SRX3177
Based on 1 Customer Validation
SRX3177 is a triple inhibitor of CDK4/6, PI3K, and BRD4, with IC50s of <2.5 nM (CDK4), 3.3 nM (CDK6), 33 nM (BRD4 BD1), 89 nM (BRD4 BD2), 79 nM (PI3Kα), 83 nM (PI3Kδ), 3.18 μM (PI3Kγ) , respectively. SRX3177 blocks the interaction between the SARS-CoV-2 E protein and the BRD2/4 BD1 domain, restores E protein-attenuated NF-κB activity. SRX3177 exerts broad cytotoxic activity against cancer cells. SRX3177 can be used for the study of anti-SARS-CoV-2 and cancer.
For research use only. We do not sell to patients.
- Purity: 99.33%
- CAS No.: 2241237-51-2
- Formula: C31H32N6O4S
- Molecular Weight:584.69
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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PI3Kα 79 nM (IC50) |
PI3Kβ 83 nM (IC50) |
PI3Kγ 3.18 μM (IC50) |
CDK4 < 2.5 nM (IC50) |
CDK6 3.3 nM (IC50) |
BRD4 (BD1) 33 nM (IC50) |
SRX3177 (0.05-20 μM, 48 h) shows a half-maximal cytotoxic concentration (CC50) of 4.57 μM in Calu-3 cells[1].
SRX3177 (0.05-20 μM, 24 h) inhibits SARS-CoV-2 Omicron replication with a half-maximal inhibitory concentration (IC50) of 0.25 μM[1].
SRX3177 reverses the diffused localization of BRD2 and restores the attenuated NF-κB activity in A549 cells with Tetracycline (HY-A0107)-inducible SARS-CoV-2 E protein[1].
SRX3177 (1 μM, 0.5-3 h) reduces c-Myc protein stability via proteasome-dependent degradation in JeKo-1 cells[1].
SRX3177 (1 μM) decreases BRD4 occupancy on c-Myc enhancer/BCL2 promoter and RNA-Pol II occupancy on c-Myc promoter in Mino cells[1].
SRX3177 (0-100 μM) displays strong antitumor activity against cyclin D1-dependent mantle cell lymphoma (Mino, Granta-519, Jeko-1), MYC-dependent neuroblastoma (CHLA-136, SMS-KNCR, CHLA-255), and PI3K-dependent hepatocellular carcinoma (HepG3, Hep3B, Huh7) cell lines, with IC50 values in nanomolar range[2].
SRX3177 (0.1-5 μM) reduces the phosphorylation levels of Rb (downstream of CDK4/6) and Akt (downstream of PI3K) in IGF-1-stimulated Huh7, CHLA-255, Jeko-1 cells [2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:JeKo-1 cells
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Concentration:1 μM
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Incubation Time:0.5, 1, 2, 3 h
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Result:Reduced c-Myc protein stability via proteasome-dependent degradation in JeKo-1 cells.
Chemical Information
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CAS No. 2241237-51-2
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Appearance Solid
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Molecular Weight 584.69
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Formula C31H32N6O4S
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Color Light yellow to brown
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SMILES
O=C1C=C(N2CCOCC2)OC3=C1SC=C3C4=CC=C(NC5=NC6=C(C=C(N6C7CCCC7)C(N(C)C)=O)C=N5)C=C4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 25 mg/mL (42.76 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (277 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
[1]. Pandey K, et al. SRX3177, a CDK4/6-PI3K-BET inhibitor, in combination with an RdRp inhibitor, Molnupiravir, or an entry inhibitor MU-UNMC-2, has potent antiviral activity against the Omicron variant of SARS-CoV-2. Antiviral Res. 2024 Jul;227:105904. [Content Brief]
[2]. Burgoyne AM, et al. A triple action CDK4/6-PI3K-BET inhibitor with augmented cancer cell cytotoxicity. Cell Discov. 2020 Jul 28;6(1):49. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7103 mL | 8.5515 mL | 17.1031 mL | 42.7577 mL |
| 5 mM | 0.3421 mL | 1.7103 mL | 3.4206 mL | 8.5515 mL | |
| 10 mM | 0.1710 mL | 0.8552 mL | 1.7103 mL | 4.2758 mL | |
| 15 mM | 0.1140 mL | 0.5701 mL | 1.1402 mL | 2.8505 mL | |
| 20 mM | 0.0855 mL | 0.4276 mL | 0.8552 mL | 2.1379 mL | |
| 25 mM | 0.0684 mL | 0.3421 mL | 0.6841 mL | 1.7103 mL | |
| 30 mM | 0.0570 mL | 0.2851 mL | 0.5701 mL | 1.4253 mL | |
| 40 mM | 0.0428 mL | 0.2138 mL | 0.4276 mL | 1.0689 mL |
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