Trk receptor

Signaling Pathway Map

Research Area

  • Inhibitory Selectivity
  • Solubility
Catalog No. Product Name Solubility(25°C)
Water DMSO Alcohol
S1124 BMS-754807 <1 mg/mL 92 mg/mL 92 mg/mL
S2891 GW441756 <1 mg/mL 25 mg/mL <1 mg/mL
S7519 GNF-5837 <1 mg/mL 100 mg/mL 9 mg/mL
S7998 Entrectinib (RXDX-101) <1 mg/mL 100 mg/mL 75 mg/mL
S7745 ANA-12 <1 mg/mL 37 mg/mL <1 mg/mL
S8511 Belizatinib (TSR-011) <1 mg/mL 100 mg/mL 100 mg/mL
S8407 PF-06273340 <1 mg/mL 95 mg/mL 1 mg/mL
S8583 TPX-0005 <1 mg/mL 70 mg/mL 10 mg/mL
S8573 Sitravatinib (MGCD516) <1 mg/mL 100 mg/mL 100 mg/mL
S8319 7,8-Dihydroxyflavone <1 mg/mL 50 mg/mL 1 mg/mL
S7960 Larotrectinib (LOXO-101) sulfate <1 mg/mL 100 mg/mL 100 mg/mL

Isoform-specific Inhibitors

Catalog No. Information Product Use Citations Product Validations
S1124

BMS-754807

BMS-754807 is a potent and reversible inhibitor of IGF-1R/InsR with IC50 of 1.8 nM/1.7 nM in cell-free assays, less potent to Met, Aurora A/B, TrkA/B and Ron, and shows little activity to Flt3, Lck, MK2, PKA, PKC etc. Phase 2.

S2891

GW441756

GW441756 is a potent, selective inhibitor of TrkA with IC50 of 2 nM, with very little activity to c-Raf1 and CDK2.

S7519

GNF-5837

GNF-5837 is a selective, and orally bioavailable pan-TRK inhibitor for TrkA, and TrkB with IC50 of 8 nM, and 12 nM, respectively.

S7998

Entrectinib (RXDX-101)

Entrectinib (RXDX-101) is an orally bioavailable pan-TrkA/B/C, ROS1 and ALK inhibitor with IC50 ranging between 0.1 and 1.7 nM. Phase 2.

S7745

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.

S8511New

Belizatinib (TSR-011)

"Belizatinib (TSR-011) is a potent inhibitor of ALK (IC50=0.7 nM) and tropomyosin receptor kinase (TRK) (IC50 values less than 3 nM for TRK A, B, and C). "

S8407New

PF-06273340

PF-06273340 is a highly potent, kinases elective, well-tolerated pan-Trk inhibitor with IC50 values of 6, 4, 3 nM for TrkA, TrkB, Trk C, respectively.

S8583New

TPX-0005

TPX-0005 is a novel ALK/ROS1/TRK inhibitor with the IC50 values of 1.01 nM for WT ALK, 1.26 nM for ALK(G1202R), and 1.08 nM for ALK(L1196M); also a potent SRC inhibitor (IC50 5.3 nM).

S8573New

Sitravatinib (MGCD516)

Sitravatinib (MGCD516) is a novel small molecule inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Kit, PDGFRβ, PDGFRα, c-Met, and Axl.

S8319

7,8-Dihydroxyflavone

7,8-Dihydroxyflavone acts as a potent and selective small-molecule agonist of the TrkB receptor (Kd ≈ 320 nM), the main signaling receptor of brain-derived neurotrophic factor (BDNF).

S7960

Larotrectinib (LOXO-101) sulfate

Larotrectinib (LOXO-101) sulfate is an oral potent and selective ATP-competitive inhibitor of tropomyosin receptor kinases (TRK).