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Trk-IN-4 (PF-6683324) is a potent pan-Trk inhibitor with IC50 = 1.1~2.6 nM for TrkA/TrkB/TrkC and antinociceptive effects. It is also a selective type II PTK6 inhibitor with IC50 = 76 nM and has antitumor effects.
Description | Trk-IN-4 (PF-6683324) is a potent pan-Trk inhibitor with IC50 = 1.1~2.6 nM for TrkA/TrkB/TrkC and antinociceptive effects. It is also a selective type II PTK6 inhibitor with IC50 = 76 nM and has antitumor effects. |
Targets&IC50 | K+ channel (hERG):14 μM, TrkC:1.1 nM, TrkA:1.9 nM, TrkB:2.6 nM |
In vitro | Trk-IN-4 is a potent pan-Trk inhibitor with cellular IC₅₀ values of 1.9 nM (TrkA), 2.6 nM (TrkB), and 1.1 nM (TrkC), showing high kinase selectivity and low hERG liability (IC₅₀ = 14 μM), with favorable lipophilic efficiency (LipE = 5.7)[1]. |
In vivo | Trk-IN-4 showed significant antinociceptive activity in a rat UV burn hyperalgesia model at oral doses of 0.03-3 mg/kg, with maximal effects at 3 mg/kg. Trk-IN-4 demonstrated good oral bioavailability (52%), low clearance, and peripheral restriction (Cb,u/Cp,u = 0.043), supporting its use as a pain therapeutic with minimal CNS side effects[1]. |
Alias | PF-6683324 |
Molecular Weight | 521.46 |
Formula | C24H23F4N5O4 |
Cas No. | 1799788-94-5 |
Smiles | O(C1=C(C(N)=O)C=C(C=N1)C=2N=CN(C)C2)[C@@H]3[C@H](F)CN(C(CC4=CC=C(OC(F)(F)F)C=C4)=O)CC3 |
Relative Density. | 1.46 g/cm3 (Predicted) |
Storage | store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice./Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 80 mg/mL (153.42 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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