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: 2 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[5] Nisha Gupta, et al. Stress granule-associated protein G3BP2 regulates breast tumor initiation
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