BPTES preferentially slows cell growth in D54 cells with mutant IDH1. BPTES also inhibits glutaminase activity, lowers glutamate and α-KG levels, and increases glycolytic intermediates.BPTES (10 μM) inhibits cell growth of mHCC 3–4 cells derived from LAP/MYC tumors. BPTES also inhibits growth of a MYC-dependent P493 cells by blocking DNA replication, leading to cell death and fragmentation.
 |
Source | Proc Natl Acad Sci U S A (2016). Figure 2. BPTES |
| Method | i.p. | |
| Cell Lines | mice | |
| Concentrations | 12.5 mg/kg | |
| Incubation Time | 3 d | |
| Results | Analysis of BPTES levels in blood, tumor, and normal pancreas by LC-MS revealed measurable drug in the tumors at 48 h postinjection (Fig. 2C), further corroborating the confocal microscopy and IVIS imaging data. |
| Molecular Weight | 524.68 |
| Formula | C24H24N6O2S3 |
| CAS Number | 314045-39-1 |
| Solubility (25°C) | DMSO 30 mg/mL warmed |
| 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.
[1] Jian Yang,et.al. Sci Rep. Targeting cellular metabolism to reduce head and neck cancer growth
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