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Compound C108 is a small molecule that exhibits cancer-selective cytotoxicity (Viability = 100%/MCF-10A vs. 50%/BT-474, 67%/4T1, 70%/MDA-MB-231 & MDA-MB-453 post 48 h 1 μM C108 treatment) and synergizes with low dose paclitaxel in reducing ALDH-positive tumor-initiating cells (TIC poulation = 56.6%/control, 60.6%/0.1 μM paclitaxel alone, 47.4%/1 μM C108 alone, 7.3%/combined treatment for 24 h in BT474 breast cancer cultures) by targeting stress granule-associated protein G3BP2 (GAP SH3 domain-binding protein 2). Likewise, C108 pretreatment prior to xenografting greatly reduces BT-474 tumor-initiating frequency (from 1/175 to 1/1103 by limiting dilution xenograft assays) in mice in vivo. G3BP2 is reported to bind and stabilize SART3 mRNA, thereby indirectly regulating the core pluripotency transcription factors Oct-4 and Nanog critically involved in ESC self-renewal and breast tumor initiation.
| Molecular Weight | 270.28 |
| Formula | C15H14N2O3 |
| CAS Number | 15533-09-2 |
| Solubility (25°C) | DMSO 22 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[5] Nisha Gupta, et al. Stress granule-associated protein G3BP2 regulates breast tumor initiation
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