Table 1.
The 50% inhibitory concentrations with their corresponding 95% confidence intervals in parenthesis of the JAK2 and PI3K inhibitors
| IC50 (μM) (95% Confidence Interval) | |||||||||
|---|---|---|---|---|---|---|---|---|---|
| TpoR JAK2 WT | TpoR JAK2 V617F | TpoR W515L | Bcr-abl | JAK2 TW | JAK2 V617F | ||||
| JAK2 inhibitors | INC424 | 4.2 (2.4–7.2) | 1.6 (1.1–2.4) | 0.1 (0.07–0.13) | 45.3 (29.9–68.7) | 1.0 (0.6–1.7) | 0.4 (0.2–0.6) | ||
| TG101348 | 1.4 (1.3–1.5) | 0.8 (0.7–0.9) | 0.8 (0.7–1.0) | 2.7 (2.2–3.3) | 1.8 (1.5–2.3) | 0.6 (0.6–0.7) | |||
| PI3K inhibitors | ZSTK474 | 225.2 (170.7–297.2) | 80.5 (56.9–113.9) | 64.3 (47.1–87.8) | 125.9 (76.7–206.4) | 250.5 (173.6–361.6) | 116.5 (99.7–136.2) | ||
| NVP-BEZ235 | 36.8 (23.9–56.6) | 3.5 (2.7–4.6) | 1.8 (1.4–2.5) | >200 | 7.5 (4.5–12.7) | 0.04 (0.02–0.06) | |||
| GDC0941 | 192.3 (127.6–289.7) | 17.9 (13.8–23.1) | 43.7 (28.3–67.6) | 147.2 (61.5–352.2) | 185.1 (165.6–206.8) | 25.8 (10.7–61.8) | |||
| TGX221 | 76.1 (67.4–86.0) | 49.4 (44.7–54.5) | 50.0 (45.9–54.6) | 75.9 (66.3–86.9) | 28.3 (15.1–53.2) | 20.39 (11.9–34.9) | |||