PT2385 inhibits expression of HIF-2α regulated genes in a dose dependent manner in vivo. Tumor is regressed with PT2385 (3 and 10 mg/kg, p.o., b.i.d. dose) in 786-O xenograft. PT2385 (1,3 and 10 mg/kg) also inhibits tumor-derived VEGFA protein levels. PT2385 (10 mg/kg) treatment reduces proliferation (Ki67) and angiogenesis (CD-31).
Oncogene. 2021 Sep;40(37):5639-5650.
Positive feedback regulation of lncRNA PVT1 and HIF2α contributes to clear cell renal cell carcinoma tumorigenesis and metastasis
PT2385 purchased from AbMole
Molecular Weight | 383.34 |
Formula | C17H12F3NO4S |
CAS Number | 1672665-49-4 |
Solubility (25°C) | DMSO: ≥ 40 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.
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