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Inhibitors
| Cat.No. | Name | Information |
|---|---|---|
| M21518 | MRTX849 ethoxypropanoic acid | LC-2 is a potent, first-in-class PROTAC capable of degrading endogenous KRAS G12C (DC50, between 0.25 and 0.76 μM). |
| M14581 | Tavilermide | Tavilermide is a selective, partial agonist of TrkA, or a nerve growth factor (NGF) mimetic. |
| M14580 | Cyclotraxin B acetate | Cyclotraxin B acetate, a cyclic peptide, is a highly potent and selective TrkB inhibitor without altering the binding of BDNF. |
| M14579 | AZ-23 | AZ-23 is an ATP-competitive and orally bioavailable Trk kinase A/B/C inhibitor with IC50s of 2 nM (TrkA), 8 nM (TrkB), 24 nM (FGFR1), 52 nM (Flt3), 55 nM (Ret), 84 nM (MuSk), 99 nM (Lck), respectively. |
| M9107 | Selitrectinib (LOXO-195) | Selitrectinib (LOXO-195) is a potent and selective, next-generation TRK inhibitor, with IC50 values of 0.6±0.1 nM, <2.5 nM for TRKA and TRKC, respectively. |
| M8106 | PF-06733804 | PF-06733804 is pan tropomyosin-related kinase (Trk) inhibitor. |
| M8105 | PF-06737007 | PF-06737007 is pan tropomyosin-related kinase (Trk) inhibitor. |
| M8104 | PF-06683324 | PF-0668324 is pan tropomyosin-related kinase (Trk) inhibitor. |
| M6211 | LOXO-101 sulfate | LOXO-101 sulfate is an oral potent and selective ATP-competitive inhibitor of tropomyosin receptor kinases (TRK). |
| M6151 | Larotrectinib (LOXO-101) | Larotrectinib (LOXO-101) is a potent, ATP competitive TRK inhibitor with IC50s in low nanomolar range for inhibition of all TRK family members in binding and cellular assays, with 100x selectivity over other kinases, with 2 to 20 nM cellular potency against the TRKA, TRKB, and TRKC kinases. |
| M5074 | ANA-12 | ANA-12 is a selective TrkB antagonist with Kd of 10 nM and 12 μM for the high and low affinity sites, respectively. |
| M2744 | GW441756 | GW441756 is a potent, selective inhibitor of TrkA with IC50 of 2 nM, with very little activity to c-Raf1 and CDK2. |
| M2585 | GNF-5837 | GNF-5837 is a potent pan-Trk inhibitor which display antiproliferative effects in cellular Ba/F3 assays (IC50 values are 7, 9 and 11 nM for cells containing the fusion proteins Tel-TrkC, Tel-TrkB and Tel-TrkA, respectively. |
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