AMG 511 is a potent and selective pan class I PI3K inhibitor, capable of inhibiting PI3K signaling and inducing robust anti-proliferative effects via a G1 arrest in many tumor cell lines, with evidence of cell killing in a subset of lines.AMG 511 is highly selective over mTOR (IC50 > 10000 nM), hVPS34 (IC50 > 9000 nM), DNAPK (IC50 = 12000 nM), and a broad panel of other protein kinases. It effectively inhibited pAKT in tumor tissue in a dose- and time-dependent manner (up to 16 hours). In animal studies it efficaciously inhibited tumor growth in PTEN-null, KRAS mutant, and HER2 amplified xenograft models. It is currently in clinical trials for cancer treatment.
| Molecular Weight | 517.6 |
| Formula | C22H28FN9O3S |
| CAS Number | 1253573-53-3 |
| Solubility (25°C) | DMSO |
| 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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