PF-06273340 is a Potent, Selective, and Peripherally Restricted Pan-Trk Inhibitor with an excellent LipE profile (IC50 value: Trk-A = 6 nM; Trk-B = 4 nM; Trk-C = 3 nM). PF-06273340 has low metabolic turnover in HLM and hHep is a good substrate for efflux transporters P-gp (ER = 35.7) and BCRP (ER = 4.0) and has moderate passive permeability (RRCK Papp = 5.4 × 10−6 cm s−1). PF-06273340 is well-tolerated was selected as a candidate for clinical development.
MedKoo Cat#: 526969
Name: PF-06273340
CAS#: 1402438-74-7
Chemical Formula: C23H22ClN7O3
Exact Mass: 479.1473
Molecular Weight: 479.93
Elemental Analysis: C, 57.56; H, 4.62; Cl, 7.39; N, 20.43; O, 10.00
| Solvent | mg/mL | mM | comments | |
|---|---|---|---|---|
| Solubility | ||||
| DMSO | 20.0 | 41.70 |
The following data is based on the product molecular weight 479.93 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
